New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors.
Bioorg Med Chem Lett
; 13(2): 175-8, 2003 Jan 20.
Article
em En
| MEDLINE
| ID: mdl-12482418
ABSTRACT
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.
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Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Receptores de Serotonina
/
Receptores de Dopamina D2
/
Receptores Adrenérgicos alfa 1
Idioma:
En
Ano de publicação:
2003
Tipo de documento:
Article