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
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