Tag: 282.2331

Brink, Christiaan B. et al. published their research in Journal of Pharmacology and Experimental Therapeutics in 2000 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Electric Literature of C10H17Cl2N3S

Agonist-directed trafficking of porcine α2A-adrenergic receptor signaling in Chinese hamster ovary cells: l-isoproterenol selectively activates Gs was written by Brink, Christiaan B.;Wade, Susan M.;Neubig, Richard R.. And the article was included in Journal of Pharmacology and Experimental Therapeutics in 2000.Electric Literature of C10H17Cl2N3S This article mentions the following:

In this study, we investigated the hypothesis of agonist-directed trafficking of receptor signaling for the α2A-adrenergic receptor (α2A-AR). α2A-ARs couple to both Gs and Gi to stimulate or inhibit adenylyl cyclase activity. Chinese hamster ovary-K1 cell lines expressing the porcine α2A-AR at high (α2A-H) and low (α2A-L) levels were used to estimate the relative efficacies (R.e.s) of a series of agonists for the Gs and Gi pathways. Gs-mediated responses were measured after pertussis toxin treatment to inactivate Gi in α2A-H, whereas Gi responses were measured in α2A-L, where Gs responses were absent. The full agonist UK-14,304 showed a large receptor reserve for Gi responses in α2A-H but little receptor reserve for Gs responses in α2A-H or for Gi responses in α2A-L. With the exception of l-isoproterenol (ISO), all agonists showed similar R.e.s. at the α2A-AR for Gs and Gi responses, with rank orders of R.e.s as follows: l-epinephrine = l-norepinephrine = UK-14,304 > p-aminoclonidine ≥ BHT-920 ≥ BHT-933 > clonidine = p-iodoclonidine ≥ xylazine ≥ guanabenz. Interestingly, ISO had the highest efficacy at the α2A-AR for activating Gs vs. Gi (9-fold higher); however, it had low potency for both. By several criteria, the ISO response was mediated by the α2A-AR, supporting the hypothesis of agonist-directed trafficking of receptor signaling or agonist-specific G protein selectivity. In contrast, the apparent Gi pathway selectivity of oxymetazoline appears to be mediated by an endogenous serotonergic receptor. It is intriguing that a classic β-AR agonist that activates Gs through β2-ARs also appears to produce a Gs-selective conformation of the Gi-coupled α2A-AR. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Electric Literature of C10H17Cl2N3S).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Electric Literature of C10H17Cl2N3S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Brink, Christiaan B. et al. published their research in Journal of Pharmacology and Experimental Therapeutics in 2000 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Electric Literature of C10H17Cl2N3S

Agonist-directed trafficking of porcine α2A-adrenergic receptor signaling in Chinese hamster ovary cells: l-isoproterenol selectively activates Gs was written by Brink, Christiaan B.;Wade, Susan M.;Neubig, Richard R.. And the article was included in Journal of Pharmacology and Experimental Therapeutics in 2000.Electric Literature of C10H17Cl2N3S This article mentions the following:

In this study, we investigated the hypothesis of agonist-directed trafficking of receptor signaling for the α2A-adrenergic receptor (α2A-AR). α2A-ARs couple to both Gs and Gi to stimulate or inhibit adenylyl cyclase activity. Chinese hamster ovary-K1 cell lines expressing the porcine α2A-AR at high (α2A-H) and low (α2A-L) levels were used to estimate the relative efficacies (R.e.s) of a series of agonists for the Gs and Gi pathways. Gs-mediated responses were measured after pertussis toxin treatment to inactivate Gi in α2A-H, whereas Gi responses were measured in α2A-L, where Gs responses were absent. The full agonist UK-14,304 showed a large receptor reserve for Gi responses in α2A-H but little receptor reserve for Gs responses in α2A-H or for Gi responses in α2A-L. With the exception of l-isoproterenol (ISO), all agonists showed similar R.e.s. at the α2A-AR for Gs and Gi responses, with rank orders of R.e.s as follows: l-epinephrine = l-norepinephrine = UK-14,304 > p-aminoclonidine ≥ BHT-920 ≥ BHT-933 > clonidine = p-iodoclonidine ≥ xylazine ≥ guanabenz. Interestingly, ISO had the highest efficacy at the α2A-AR for activating Gs vs. Gi (9-fold higher); however, it had low potency for both. By several criteria, the ISO response was mediated by the α2A-AR, supporting the hypothesis of agonist-directed trafficking of receptor signaling or agonist-specific G protein selectivity. In contrast, the apparent Gi pathway selectivity of oxymetazoline appears to be mediated by an endogenous serotonergic receptor. It is intriguing that a classic β-AR agonist that activates Gs through β2-ARs also appears to produce a Gs-selective conformation of the Gi-coupled α2A-AR. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Electric Literature of C10H17Cl2N3S).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Electric Literature of C10H17Cl2N3S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sharma, Alok et al. published their research in Indian Journal of Experimental Biology in 1994 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Reference of 36085-73-1

Dopamine receptor mediated antidepressant action of B-HT 920 in mice was written by Sharma, Alok;Kulkarni, S K.. And the article was included in Indian Journal of Experimental Biology in 1994.Reference of 36085-73-1 This article mentions the following:

Possible involvement of dopaminergic (DAergic) system in forced swimming-induced immobility (despair behavior) was investigated in mice. B-HT 920 (0.05 and 0.1 mg/kg), a post-synaptic DAergic agonist, produced a dose dependent reduction in immobility period, which was sensitive to blockade by haloperidol (0.5 mg/kg) and sulpiride (100 mg/kg). This effect was also blocked by 伪2 antagonist yohimbine (5 mg/kg). SKF 38393 (5 mg/kg), a D1-DA agonist potentiated the action of B-HT 920. Reserpinization (2 mg/kg, 24 h prior) produced despair immobility in mice. When a low dose of B-HT 920 (0.05 mg/kg) was given to reserpinized animals, the duration of immobility period was further increased. But on the other hand, a higher dose (0.1 mg/kg) of it reduced reserpine-induced immobility. Desipramine (5 and 10 mg/kg), elicited a dose dependent reduction in the immobility period, which was sensitive to blockade by sulpiride (100 mg/kg). Desipramine (10 mg/kg) showed a biphasic response in combination with B-HT 920, i.e., a potentiation of the response due to a low dose of B-HT 920 (0.05 mg/kg) and an antagonism of the response due to a higher dose of B-HT 920 (0.1 mg/kg), resp. SKF 38393 (5 mg/kg), potentiated the action of desipramine (5 mg/kg). SKF 38393 (5 mg/kg) further potentiated the action of desipramine (5 mg/kg) and B-HT 920 (0.05 mg/kg). These observations suggests that B-HT 920 reduces behavioral immobility by DAergic mechanism and desipramine also modulates D2-DA receptors in its anti-depressant action. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Reference of 36085-73-1).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Reference of 36085-73-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Pauwels, P. J. et al. published their research in Biochemical Pharmacology in 2001 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride

Modulation of ligand responses by coupling of 伪2A-adrenoceptors to diverse G伪-proteins was written by Pauwels, P. J.;Tardif, S.;Colpaert, F. C.;Wurch, T.. And the article was included in Biochemical Pharmacology in 2001.Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride This article mentions the following:

The hypothesis that different signaling may be mediated via a single 伪2A-adrenoceptor (伪2A AR) subtype was investigated by challenging 伪2 AR ligands in combination with diverse recombinant weight, mutant, and chimeric G伪-proteins. Possible coupling of 伪2A AR to endogenous G伪i/o-proteins in CHO-K1 cells was excluded by measuring pertussis toxin (PTX)-resistant [35S]GTP纬S-binding responses as a common functional response to 伪2A AR activation. (-)-Adrenaline (10 渭M) displayed the highest magnitude of [35S]GTP纬S-binding response in the co-presence of a PTX-resistant G伪oCys351Ile protein, whereas a decreased response was obtained with the mutant G伪i1/2-proteins. Replacement of the last six amino acids at the C-terminal portion of the G伪o-protein by the corresponding amino acid region of either the G伪z-, G伪s-, G伪q-, or G伪15-protein and co-expression with the 伪2A AR resulted in similar maximal (-)-adrenaline-mediated [35S]GTP纬S-binding responses with these chimeric G伪o-proteins. The ligands D-medetomidine, BHT 920 (6-allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-ylamine) and (+)-RX 811059 (2-(2-ethoxy-2,3-dihydro-benzo[1,4]dioxin-2-yl)-4,5-dihydro-1H-imidazole) were weakly active or virtually inactive at the chimeric G伪o/s-, G伪o/q-, and G伪o/15-proteins in contrast to the G伪o/z-protein. Furthermore, combining the constitutively active mutant Thr373Lys 伪2A AR with these chimeric G伪o-proteins enhanced the apparent intrinsic activity of D-medetomidine and BHT 920. A similar observation was made using the corresponding fusion proteins, where the stoichiometry of the mutant 伪2A AR to the chimeric G伪o-protein was fixed at 1.0. These data indicate that a single ligand may display different magnitudes of activation at the 伪2A AR subtype coupled to chimeric G伪o proteins under controlled conditions of 伪2A AR: G伪o-protein expression. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Otvos, Reka A. et al. published their research in Toxins in 2015 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Product Details of 36085-73-1

Development of plate reader and on-line microfluidic screening to identify ligands of the 5-hydroxytryptamine binding protein in venoms was written by Otvos, Reka A.;Iyer, Janaki Krishnamoorthy;van Elk, Rene;Ulens, Chris;Niessen, Wilfried M. A.;Somsen, Govert W.;Manjunatha, Kini R.;Smit, August B.;Kool, Jeroen. And the article was included in Toxins in 2015.Product Details of 36085-73-1 This article mentions the following:

The 5-HT3 receptor is a ligand-gated ion channel, which is expressed in the nervous system. Its antagonists are used clin. for treatment of postoperative- and radiotherapy-induced emesis and irritable bowel syndrome. In order to better understand the structure and function of the 5-HT3 receptor, and to allow for compound screening at this receptor, recently a serotonin binding protein (5HTBP) was engineered with the Acetylcholine Binding Protein as template. In this study, a fluorescence enhancement assay for 5HTBP ligands was developed in plate-reader format and subsequently used in an online microfluidic format. Both assay types were validated using an existing radioligand binding assay. The online microfluidic assay was coupled to HPLC via a post-column split which allowed parallel coupling to a mass spectrometer to collect MS data. This high-resolution screening (HRS) system is well suitable for compound mixture anal. As a proof of principle, the venoms of Dendroapsis polylepis, Pseudonaja affinis and Pseudonaja inframacula snakes were screened and the accurate masses of the found bioactives were established. To demonstrate the subsequent workflow towards structural identification of bioactive proteins and peptides, the partial amino acid sequence of one of the bioactives from the Pseudonaja affinis venom was determined using a bottom-up proteomics approach. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Product Details of 36085-73-1).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Product Details of 36085-73-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Molderings, G. J. et al. published their research in Naunyn-Schmiedeberg’s Archives of Pharmacology in 1995 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Category: thiazole

Subtype determination of presynaptic 伪2-autoreceptors in the rabbit pulmonary artery and human saphenous vein was written by Molderings, G. J.;Gothert, M.. And the article was included in Naunyn-Schmiedeberg’s Archives of Pharmacology in 1995.Category: thiazole This article mentions the following:

The pharmacol. properties of the presynaptic 伪2-autoreceptors mediating inhibition of noradrenaline release were investigated in human saphenous vein and rabbit pulmonary artery. Segments of these blood vessels were incubated with [3H]noradrenaline and subsequently superfused with physiol. salt solution containing uptake1 and uptake2 blockers. The potencies of 伪2-adrenoceptor antagonists in facilitating (pEC40) the elec. (2Hz) evoked tritium overflow were determined The order of potency and potency ratios of 伪2-adrenoceptor antagonists in facilitating (pEC40) the elec. (2Hz) evoked tritium overflow were determined The order of potency and potency rations of 伪2-adrenoceptor antagonists obtained in the experiments were compared with the corresponding order of affinity and affinity rations from radioligand binding studies in tissues and cells expressing only 1 of the 伪2-adrenoceptor subtypes. In the rabbit pulmonary artery, oxymetazoline was a highly potent agonist at presynaptic 伪2-adrenoceptors, as reflected by its ability to inhibit at low concentrations the elec. evoked tritium overflow. However, in the human saphenous vein oxymetazoline behaved as a partial agonist, which, interaction experiments with the 伪2-adrenoceptor agonist B-HT 920 (2-amino-6-allyl-5-6,7,8-tetrahydro-4H-thiazolo-[4,5-d]-azephine), exhibited high potency in antagonizing the inhibitory effect of the latter drug on tritium overflow. Prazosin given alone at concentrations 鈮? 渭M did not affect tritium overflow. The data obtained with oxymetazoline and prazosin make it very improbable that the 伪2-autoreceptors on the sympathetic nerves in both tissues are of the 伪2B– or 伪2C– subtype. In both blood vessels, rauwolscine given alone was highly potent in facilitating the elec. evoked overflow. In agreement with this, rauwolscine exhibited high potency in antagonizing the inhibitory effect of oxymetazoline on tritium overflow in the rabbit pulmonary artery and of B-HT 920 in the human saphenous vein. The ratio phentolamine/rauwolscine calculated from their potencies in increasing the elec. evoked tritium overflow was also used to discriminate between the various a2-adrenoceptor subtypes. Comparisons of this potency ratio with the corresponding affinity ratios for 伪2-adrenergic binding sites on HT 29 cells, human platelets, bovine pineal gland, rat submaxillary gland, and cell lines transfected with the human 伪2 genes indicates that in the rabbit pulmonary artery and human saphenous vein the pharmacol. characteristics of the autoreceptors conform best to those of 伪2A-adrenoceptors. Finally, in both blood vessels the potencies of the antagonists BDF 6143 (4-chloro-2-(2-imidazolin-2-ylamino)-isoindoline), rauwolscine, corynanthine, phentolamine, idazoxan, SKF 104078 (6-chloro-9-[(3-methyl-2-butenyl) oxyl]-3-methyl-1-1H-2,3,4,5-tetrahydro-3-benzazepine), and/or tolazoline in facilitating evoked noradrenaline, and/or tolazoline in facilitating evoked noradrenaline release was determined The potencies of these drugs which can discriminate between 伪2A– and 伪2D-adrenoceptors (but not between these and 伪2B/2C-adrenoceptors) were correlated significantly with their affinities for 伪2A, but not 伪2D, sites in radioligand binding studies. Apparently, the sympathetic nerves of the human saphenous vein and rabbit pulmonary artery are endowed with 伪2-autoreceptors of the 伪2A subtype. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Category: thiazole).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Sharma, Alok et al. published their research in Indian Journal of Experimental Biology in 1994 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Reference of 36085-73-1

Dopamine receptor mediated antidepressant action of B-HT 920 in mice was written by Sharma, Alok;Kulkarni, S K.. And the article was included in Indian Journal of Experimental Biology in 1994.Reference of 36085-73-1 This article mentions the following:

Possible involvement of dopaminergic (DAergic) system in forced swimming-induced immobility (despair behavior) was investigated in mice. B-HT 920 (0.05 and 0.1 mg/kg), a post-synaptic DAergic agonist, produced a dose dependent reduction in immobility period, which was sensitive to blockade by haloperidol (0.5 mg/kg) and sulpiride (100 mg/kg). This effect was also blocked by α2 antagonist yohimbine (5 mg/kg). SKF 38393 (5 mg/kg), a D1-DA agonist potentiated the action of B-HT 920. Reserpinization (2 mg/kg, 24 h prior) produced despair immobility in mice. When a low dose of B-HT 920 (0.05 mg/kg) was given to reserpinized animals, the duration of immobility period was further increased. But on the other hand, a higher dose (0.1 mg/kg) of it reduced reserpine-induced immobility. Desipramine (5 and 10 mg/kg), elicited a dose dependent reduction in the immobility period, which was sensitive to blockade by sulpiride (100 mg/kg). Desipramine (10 mg/kg) showed a biphasic response in combination with B-HT 920, i.e., a potentiation of the response due to a low dose of B-HT 920 (0.05 mg/kg) and an antagonism of the response due to a higher dose of B-HT 920 (0.1 mg/kg), resp. SKF 38393 (5 mg/kg), potentiated the action of desipramine (5 mg/kg). SKF 38393 (5 mg/kg) further potentiated the action of desipramine (5 mg/kg) and B-HT 920 (0.05 mg/kg). These observations suggests that B-HT 920 reduces behavioral immobility by DAergic mechanism and desipramine also modulates D2-DA receptors in its anti-depressant action. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Reference of 36085-73-1).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Reference of 36085-73-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Pauwels, P. J. et al. published their research in Biochemical Pharmacology in 2001 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride

Modulation of ligand responses by coupling of α2A-adrenoceptors to diverse Gα-proteins was written by Pauwels, P. J.;Tardif, S.;Colpaert, F. C.;Wurch, T.. And the article was included in Biochemical Pharmacology in 2001.Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride This article mentions the following:

The hypothesis that different signaling may be mediated via a single α2A-adrenoceptor (α2A AR) subtype was investigated by challenging α2 AR ligands in combination with diverse recombinant weight, mutant, and chimeric Gα-proteins. Possible coupling of α2A AR to endogenous Gαi/o-proteins in CHO-K1 cells was excluded by measuring pertussis toxin (PTX)-resistant [35S]GTPγS-binding responses as a common functional response to α2A AR activation. (-)-Adrenaline (10 μM) displayed the highest magnitude of [35S]GTPγS-binding response in the co-presence of a PTX-resistant GαoCys351Ile protein, whereas a decreased response was obtained with the mutant Gαi1/2-proteins. Replacement of the last six amino acids at the C-terminal portion of the Gαo-protein by the corresponding amino acid region of either the Gαz-, Gαs-, Gαq-, or Gα15-protein and co-expression with the α2A AR resulted in similar maximal (-)-adrenaline-mediated [35S]GTPγS-binding responses with these chimeric Gαo-proteins. The ligands D-medetomidine, BHT 920 (6-allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-ylamine) and (+)-RX 811059 (2-(2-ethoxy-2,3-dihydro-benzo[1,4]dioxin-2-yl)-4,5-dihydro-1H-imidazole) were weakly active or virtually inactive at the chimeric Gαo/s-, Gαo/q-, and Gαo/15-proteins in contrast to the Gαo/z-protein. Furthermore, combining the constitutively active mutant Thr373Lys α2A AR with these chimeric Gαo-proteins enhanced the apparent intrinsic activity of D-medetomidine and BHT 920. A similar observation was made using the corresponding fusion proteins, where the stoichiometry of the mutant α2A AR to the chimeric Gαo-protein was fixed at 1.0. These data indicate that a single ligand may display different magnitudes of activation at the α2A AR subtype coupled to chimeric Gαo proteins under controlled conditions of α2A AR: Gαo-protein expression. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Application In Synthesis of 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Otvos, Reka A. et al. published their research in Toxins in 2015 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Product Details of 36085-73-1

Development of plate reader and on-line microfluidic screening to identify ligands of the 5-hydroxytryptamine binding protein in venoms was written by Otvos, Reka A.;Iyer, Janaki Krishnamoorthy;van Elk, Rene;Ulens, Chris;Niessen, Wilfried M. A.;Somsen, Govert W.;Manjunatha, Kini R.;Smit, August B.;Kool, Jeroen. And the article was included in Toxins in 2015.Product Details of 36085-73-1 This article mentions the following:

The 5-HT3 receptor is a ligand-gated ion channel, which is expressed in the nervous system. Its antagonists are used clin. for treatment of postoperative- and radiotherapy-induced emesis and irritable bowel syndrome. In order to better understand the structure and function of the 5-HT3 receptor, and to allow for compound screening at this receptor, recently a serotonin binding protein (5HTBP) was engineered with the Acetylcholine Binding Protein as template. In this study, a fluorescence enhancement assay for 5HTBP ligands was developed in plate-reader format and subsequently used in an online microfluidic format. Both assay types were validated using an existing radioligand binding assay. The online microfluidic assay was coupled to HPLC via a post-column split which allowed parallel coupling to a mass spectrometer to collect MS data. This high-resolution screening (HRS) system is well suitable for compound mixture anal. As a proof of principle, the venoms of Dendroapsis polylepis, Pseudonaja affinis and Pseudonaja inframacula snakes were screened and the accurate masses of the found bioactives were established. To demonstrate the subsequent workflow towards structural identification of bioactive proteins and peptides, the partial amino acid sequence of one of the bioactives from the Pseudonaja affinis venom was determined using a bottom-up proteomics approach. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Product Details of 36085-73-1).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Product Details of 36085-73-1

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Molderings, G. J. et al. published their research in Naunyn-Schmiedeberg’s Archives of Pharmacology in 1995 | CAS: 36085-73-1

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Category: thiazole

Subtype determination of presynaptic α2-autoreceptors in the rabbit pulmonary artery and human saphenous vein was written by Molderings, G. J.;Gothert, M.. And the article was included in Naunyn-Schmiedeberg’s Archives of Pharmacology in 1995.Category: thiazole This article mentions the following:

The pharmacol. properties of the presynaptic α2-autoreceptors mediating inhibition of noradrenaline release were investigated in human saphenous vein and rabbit pulmonary artery. Segments of these blood vessels were incubated with [3H]noradrenaline and subsequently superfused with physiol. salt solution containing uptake1 and uptake2 blockers. The potencies of α2-adrenoceptor antagonists in facilitating (pEC40) the elec. (2Hz) evoked tritium overflow were determined The order of potency and potency ratios of α2-adrenoceptor antagonists in facilitating (pEC40) the elec. (2Hz) evoked tritium overflow were determined The order of potency and potency rations of α2-adrenoceptor antagonists obtained in the experiments were compared with the corresponding order of affinity and affinity rations from radioligand binding studies in tissues and cells expressing only 1 of the α2-adrenoceptor subtypes. In the rabbit pulmonary artery, oxymetazoline was a highly potent agonist at presynaptic α2-adrenoceptors, as reflected by its ability to inhibit at low concentrations the elec. evoked tritium overflow. However, in the human saphenous vein oxymetazoline behaved as a partial agonist, which, interaction experiments with the α2-adrenoceptor agonist B-HT 920 (2-amino-6-allyl-5-6,7,8-tetrahydro-4H-thiazolo-[4,5-d]-azephine), exhibited high potency in antagonizing the inhibitory effect of the latter drug on tritium overflow. Prazosin given alone at concentrations ≤1 μM did not affect tritium overflow. The data obtained with oxymetazoline and prazosin make it very improbable that the α2-autoreceptors on the sympathetic nerves in both tissues are of the α2B– or α2C– subtype. In both blood vessels, rauwolscine given alone was highly potent in facilitating the elec. evoked overflow. In agreement with this, rauwolscine exhibited high potency in antagonizing the inhibitory effect of oxymetazoline on tritium overflow in the rabbit pulmonary artery and of B-HT 920 in the human saphenous vein. The ratio phentolamine/rauwolscine calculated from their potencies in increasing the elec. evoked tritium overflow was also used to discriminate between the various a2-adrenoceptor subtypes. Comparisons of this potency ratio with the corresponding affinity ratios for α2-adrenergic binding sites on HT 29 cells, human platelets, bovine pineal gland, rat submaxillary gland, and cell lines transfected with the human α2 genes indicates that in the rabbit pulmonary artery and human saphenous vein the pharmacol. characteristics of the autoreceptors conform best to those of α2A-adrenoceptors. Finally, in both blood vessels the potencies of the antagonists BDF 6143 (4-chloro-2-(2-imidazolin-2-ylamino)-isoindoline), rauwolscine, corynanthine, phentolamine, idazoxan, SKF 104078 (6-chloro-9-[(3-methyl-2-butenyl) oxyl]-3-methyl-1-1H-2,3,4,5-tetrahydro-3-benzazepine), and/or tolazoline in facilitating evoked noradrenaline, and/or tolazoline in facilitating evoked noradrenaline release was determined The potencies of these drugs which can discriminate between α2A– and α2D-adrenoceptors (but not between these and α2B/2C-adrenoceptors) were correlated significantly with their affinities for α2A, but not α2D, sites in radioligand binding studies. Apparently, the sympathetic nerves of the human saphenous vein and rabbit pulmonary artery are endowed with α2-autoreceptors of the α2A subtype. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Category: thiazole).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Category: thiazole

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica