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  • Title: Ligands for the investigation of 5-HT autoreceptor function.
    Author: Roberts C, Price GW, Middlemiss DN.
    Journal: Brain Res Bull; 2001 Nov 15; 56(5):463-9. PubMed ID: 11750791.
    Abstract:
    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.
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