BRL-15,572 explained

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.[1] [2] One function of the 5-HT1D receptor this research has revealed is its role in modulating release of the neurotransmitter glutamate in the brain,[3] as well as functions in regulation of cerebral blood pressure which are important in the pathogenesis of migraine headaches.[4]

Notes and References

  1. Price GW, Burton MJ, Collin LJ, Duckworth M, Gaster L, Göthert M, Jones BJ, Roberts C, Watson JM, Middlemiss DN . 6 . 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 . September 1997 . 9303567 . 10.1007/pl00005056 . 26760453 .
  2. Schlicker E, Fink K, Molderings GJ, Price GW, Duckworth M, Gaster L, Middlemiss DN, Zentner J, Likungu J, Göthert M . 6 . 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 . September 1997 . 9303568 . 10.1007/pl00005057 . 12246022 .
  3. 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 . 126 . 3 . 607–12 . February 1999 . 10188970 . 1565844 . 10.1038/sj.bjp.0702336 .
  4. 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 . 122 . 2 . 491–8 . 14614913 . 10.1016/s0306-4522(03)00570-0 . 2003 . 24825348 .

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