期刊
MOLECULAR PHARMACOLOGY
卷 75, 期 6, 页码 1380-1391出版社
AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS
DOI: 10.1124/mol.108.054395
关键词
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资金
- Ministerio de Educacion y Ciencia, Spain [SAF2007-65913, SAF2005-08025-C03]
- Xunta de Galicia [PGIDIT06PXID203186PR, 2007/118]
- Instituto de Salud Carlos III
- Fundacio La Marato de TV3 [070530]
The serotonin (5-hydroxytryptamine; 5-HT) 2A receptor is a cell surface class A G protein-coupled receptor that regulates a multitude of physiological functions of the body and is a target for antipsychotic drugs. Here we found by means of fluorescence resonance energy transfer and immunoprecipitation studies that the 5-HT2A-receptor homodimerized in live cells, which we linked with its antagonist-dependent fingerprint in both binding and receptor signaling. Some antagonists, like the atypical antipsychotics clozapine and risperidone, differentiate themselves from others, like the typical antipsychotic haloperidol, antagonizing these 5-HT2A receptor-mediated functions in a pathway-specific manner, explained here by a new model of multiple active interconvertible conformations at dimeric receptors.
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