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BRL-15,572
BRL-15,572 is a drug which acts as a selective antagonist for the serotonin receptor subtype 5-HT1D, with around 60x selectivity over other related receptors. The 5-HT1D receptor has a very similar pharmacology to the closely related 5-HT1B receptor, and most older ligands for these receptors bind to both subtypes with approximately equal affinity, so development of compounds such as BRL-15572 which are able to selectively block the 5-HT1D subtype while leaving 5-HT1B unaffected, have been a significant advance which has helped scientists in researching the function of these serotonin receptor subtypes.〔Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN. SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors. ''Naunyn Schmiedebergs Archives of Pharmacology''. 1997 Sep;356(3):312-20. PMID 9303567〕〔Schlicker E, Fink K, Molderings GJ, Price GW, Duckworth M, Gaster L, Middlemiss DN, Zentner J, Likungu J, Göthert M. Effects of selective h5-HT1B (SB-216641) and h5-HT1D (BRL-15572) receptor ligands on guinea-pig and human 5-HT auto- and heteroreceptors. ''Naunyn Schmiedebergs Archives of Pharmacology''. 1997 Sep;356(3):321-7. PMID 9303568〕 One function of the 5-HT1D receptor this research has revealed is its role in modulating release of the neurotransmitter glutamate in the brain,〔Marcoli M, Maura G, Munari C, Ruelle A, Raiteri M. Pharmacological diversity between native human 5-HT1B and 5-HT1D receptors sited on different neurons and involved in different functions. ''British Journal of Pharmacology''. 1999 Feb;126(3):607-12. PMID 10188970〕 as well as functions in regulation of cerebral blood pressure which are important in the pathogenesis of migraine headaches.〔Goadsby PJ, Classey JD. Evidence for serotonin (5-HT)1B, 5-HT1D and 5-HT1F receptor inhibitory effects on trigeminal neurons with craniovascular input. ''Neuroscience''. 2003;122(2):491-8. PMID 14614913〕
== References ==
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