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

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