Document Detail

Studies on 1-arylpiperazine derivatives with affinity for rat 5-HT7 and 5-HT1A receptors.
MedLine Citation:
PMID:  15005884     Owner:  NLM     Status:  MEDLINE    
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.
Marcello Leopoldo; Francesco Berardi; Nicola A Colabufo; Marialessandra Contino; Enza Lacivita; Roberto Perrone; Vincenzo Tortorella
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  56     ISSN:  0022-3573     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  2004 Feb 
Date Detail:
Created Date:  2004-03-09     Completed Date:  2004-06-23     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  247-55     Citation Subset:  IM    
Dipartimento Farmaco-Chimico, Università degli Studi di Bari, via Orabona, 4, 70125 Bari, Italy.
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MeSH Terms
Cell Line
Gene Transfer Techniques
Guinea Pigs
Hippocampus / cytology,  drug effects
Ileum / drug effects
Kidney / cytology
Membranes / cytology,  drug effects
Piperazines / chemical synthesis*,  pharmacokinetics*
Quantitative Structure-Activity Relationship
Radioligand Assay
Rats, Wistar
Receptor, Serotonin, 5-HT1A / drug effects*,  genetics
Receptors, Serotonin / drug effects*
Serotonin Agonists / chemical synthesis,  pharmacokinetics
Reg. No./Substance:
0/Piperazines; 0/Receptors, Serotonin; 0/Serotonin Agonists; 0/serotonin 7 receptor; 112692-38-3/Receptor, Serotonin, 5-HT1A

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