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BRL-15,572

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BRL-15,572
Clinical data
ATC code
  • none
Identifiers
  • 3-(4-(4-chlorophenyl)piperazin-1-yl)-1,1-diphenyl-2-propanol
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC25H27ClN2O
Molar mass406.947 g/mol g·mol−1
3D model (JSmol)
  • Clc2cccc(c2)N1CCN(CC1)CC(O)C(c3ccccc3)c4ccccc4
 ☒NcheckY (what is this?)  (verify)

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]

References

  1. ^ 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
  2. ^ 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
  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. 1999 Feb;126(3):607-12. PMID 10188970
  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. 2003;122(2):491-8. PMID 14614913


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