New Arylpiperazine Derivatives with High Affinity for α1A, D2 and 5-HT2A Receptors
| Autor: | Jose C. Gonzalez‐Gomez, M. De Luca, Eugenio Uriarte, José Angel Fontenla, M. E. Rivas, M. Villazon, José Brea, María Isabel Loza, Lourdes Santana, G. Y. Montenegro |
|---|---|
| Rok vydání: | 2003 |
| Předmět: |
Male
5-HT2A receptor Stereochemistry Clinical Biochemistry Pharmaceutical Science Aorta Thoracic In Vitro Techniques Ring (chemistry) Biochemistry Chemical synthesis Muscle Smooth Vascular Piperazines Rats Sprague-Dawley Structure-Activity Relationship chemistry.chemical_compound Coumarins Receptors Adrenergic alpha-1 Drug Discovery Haloperidol medicine Animals Receptor Serotonin 5-HT2A Receptor Molecular Biology Arylpiperazine derivatives chemistry.chemical_classification Receptors Dopamine D2 Organic Chemistry General Medicine Coumarin In vitro Rats Piperazine chemistry Receptors Serotonin Dopamine Antagonists Molecular Medicine Indicators and Reagents Algorithms Lactone medicine.drug |
| Zdroj: | ChemInform. 34 |
| ISSN: | 1522-2667 0931-7597 |
| DOI: | 10.1002/chin.200317136 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Plný text