BRL-15,572 is a
drug which acts as a
selectiveantagonist for the
serotoninreceptor 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.[1][2] One function of the 5-HT1D receptor this research has revealed is its role in modulating release of the
neurotransmitterglutamate in the brain,[3] as well as functions in regulation of cerebral blood pressure which are important in the pathogenesis of
migraine headaches.[4]
References
^Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, et al. (September 1997). "SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 356 (3): 312–20.
doi:
10.1007/pl00005056.
PMID9303567.
S2CID26760453.
^Schlicker E, Fink K, Molderings GJ, Price GW, Duckworth M, Gaster L, et al. (September 1997). "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-Schmiedeberg's Archives of Pharmacology. 356 (3): 321–7.
doi:
10.1007/pl00005057.
PMID9303568.
S2CID12246022.
BRL-15,572 is a
drug which acts as a
selectiveantagonist for the
serotoninreceptor 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.[1][2] One function of the 5-HT1D receptor this research has revealed is its role in modulating release of the
neurotransmitterglutamate in the brain,[3] as well as functions in regulation of cerebral blood pressure which are important in the pathogenesis of
migraine headaches.[4]
References
^Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, et al. (September 1997). "SB-216641 and BRL-15572--compounds to pharmacologically discriminate h5-HT1B and h5-HT1D receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 356 (3): 312–20.
doi:
10.1007/pl00005056.
PMID9303567.
S2CID26760453.
^Schlicker E, Fink K, Molderings GJ, Price GW, Duckworth M, Gaster L, et al. (September 1997). "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-Schmiedeberg's Archives of Pharmacology. 356 (3): 321–7.
doi:
10.1007/pl00005057.
PMID9303568.
S2CID12246022.