| 15005884 |
Leopoldo M, Berardi F, Colabufo NA, Contino M, Lacivita E, Perrone R, Tortorella V: Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors. J Pharm Pharmacol. 2004 Feb;56(2):247-55.
Several 1-aryl-4-(2-arylethyl) piperazine derivatives were synthesized and tested in-vitro for their binding affinity for 5-HT (7) and 5-HT (1A) receptors. These compounds displayed 5-HT (7 ) receptor affinity ranging between K (i) = 474 nM and K (i) = 8.2 nM, besides high affinity for the 5-HT (1A) receptor. Intrinsic activity of the most potent compounds was assessed. 4-[2-(3-Methoxyphenyl) ethyl]-1-(2-methoxyphenyl) piperazine (16) and 1-(1,2-benzisoxazol-3-yl)-4-[2-(3-methoxyphenyl) ethyl] piperazine (20) (K (i) = 24.5 and 8.2 nM, respectively) behaved as partial agonist and full agonist, respectively, when tested for 5-HT (7) receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction. |
83(1,1,1,3) |