Ligands for the investigation of 5-HT autoreceptor function.
The existence of multiple 5-HT autoreceptors in the central nervous system is now firmly established and they have been pharmacologically identified as belonging to the 5-HT(1A), 5-HT(1B), and 5-HT(1D) receptor subtypes. In addition, 5-HT(1F), 5-HT(5A), and 5-HT(7) receptors remain as potential candidates for additional autoreceptors. The emergence of selective ligands, such as SB-224289 (5-HT(1B) receptor antagonist), BRL 15572 (5-HT(1D) receptor antagonist), GR 127935 (a mixed 5-HT(1B/1D) receptor antagonist), LY 334370 (5-HT(1F) receptor agonist), and SB-269970 (5-HT(7) receptor antagonist), has aided the characterisation of 5-HT autoreceptors and has highlighted the complexity of mechanisms which modulate the release of 5-HT.
Roberts
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C
Neuroscience Research, GlaxoSmithKline, Harlow, Essex, UK. claire_roberts-1@gsk.com
Price
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Middlemiss
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DN
D000818:Animals; D017660:Autoreceptors / Q000187:drug effects / Q000378:metabolism*; D002490:Central Nervous System / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D008024:Ligands; D009474:Neurons / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D017729:Presynaptic Terminals / Q000187:drug effects / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000494:pharmacology*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*
D017660:Autoreceptors; D008024:Ligands; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D012701:Serotonin