| Name | alpha adrenoceptor |
|---|---|
| Synonyms | Alpha 2A Adrenoceptor; ZNF32; ADRA2; ADRA2A; ADRA2R; ADRAR; ALPHA2AAR; Alpha 2A adrenergic receptor… |
| Name | cyanamide |
|---|---|
| CAS | cyanamide |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 6125596 | Chapleo CB, Doxey JC, Myers PL: Synthesis of some potential antihypertensive phthalazinyl- and quinoxalinylguanidines. J Med Chem. 1982 Jul;25(7):821-4. Substituted guanidines were prepared by treating the cyanamides 9 and 16 with the appropriate amine; with hydrazines, cyanamide 9 gave the triazoles 14 and 15. Some of the compounds (10, 11, 13, and 18) displayed weak alpha-adrenoceptor antagonist properties in vitro, and this activity was confirmed in the pithed rat (in vivo). |
1(0,0,0,1) | Details |
| 2896246 | Bordner J, Campbell SF, Palmer MJ, Tute MS: 1,3-Diamino-6,7-dimethoxyisoquinoline derivatives as potential alpha 1-adrenoceptor antagonists. J Med Chem. 1988 May;31(5):1036-9. Treatment of 2-methyl-4,5-dimethoxybenzonitrile (3) with LDA followed by reaction with an N,N-disubstituted cyanamide provided a series of 1,3-diamino-6,7-dimethoxyisoquinolines (2), which were evaluated for alpha-adrenoceptor binding affinity and antihypertensive activity. 1-Amino-3-(dimethylamino)-6,7-dimethoxyisoquinoline (4) showed no significant affinity (Ki much greater than 10 (-6) M) for alpha 1-adrenoceptors, while the corresponding 3-(2-furoylpiperazin-1-yl) analogue (8; Ki = 1.6 X 10 (-7) M) was some 1000-fold less potent than prazosin. pKa data showed that N-2 protonation (34%) of 4 (pKa = 7.1) would occur at physiological pH, in agreement with X-ray crystallographic analysis of 8.HCl. |
0(0,0,0,0) | Details |