| 12482418 |
Gonzalez-Gomez JC, Santana L, Uriarte E, Brea J, Villazon M, Loza MI, De Luca M, Rivas ME, Montenegro GY, Fontenla JA: New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors. Bioorg Med Chem Lett. 2003 Jan 20;13(2):175-8.
A series of novel long-chain arylpiperazines bearing a coumarin fragment was synthesized and the compounds were evaluated for their affinity at alpha (1), D (2 ) and 5-HT (2A) receptors. Most of the new compounds showed high affinity for the three types of receptors alpha (1A), D (2) and 5-HT (2A) which depends, fundamentally, on the substitution of the N (4) of the piperazine ring. From the series emerged compound 6, which had an haloperidol-like profile at D (2) and 5HT (2A) receptors (pK (i) values of 7.93 and 6.76 respectively). The higher alpha (1A) receptor affinity (pA (2)=9.07) of this compound could contribute to a more atypical antipsychotic profile than the haloperidol. |
33(0,1,1,3) |