Pharmacological differentiation of human 5-HT1B and 5-HT1D receptors.
Human 5-hydroxytryptamine1B (5-HT1B; also designated 5-HT1D beta) receptors and 5-HT1D (also designated 5-HT1D alpha) receptors are distinct molecular entities which mediate serotonergic neurotransmission. The often confusing variability in nomenclature for these two G protein-coupled receptors derives from a preliminary observation that these receptors display nearly indistinguishable pharmacological properties. The present study analyzed a series of 21 drugs, 8 of which were found to be at least an order of magnitude more potent at 5-HT1D than 5-HT1B receptors. These data provide pharmacological evidence that human 5-HT1B and 5-HT1D receptors are distinct molecular entities which represent independent targets for future drug development. Furthermore, these data indicate that a number of selective pharmacological agents already exist and can be used to analyze the functional roles of 5-HT1B and 5-HT1D receptors.
Peroutka
S J
SJ
Palo Alto Institute for Molecular Medicine, Burlingame, CA 94010-7429.
D002460:Cell Line; D004087:Dihydroergotamine / Q000494:pharmacology; D004347:Drug Interactions; D004878:Ergotamine / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D011985:Receptors, Serotonin / Q000145:classification* / Q000187:drug effects* / Q000502:physiology; D012701:Serotonin / Q000031:analogs & derivatives / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000494:pharmacology; D015398:Signal Transduction
D011985:Receptors, Serotonin; D017366:Serotonin Receptor Agonists; D012701:Serotonin; D004087:Dihydroergotamine; C047087:5-carboxamidotryptamine; D004878:Ergotamine