BRL-15,572

BRL-15,572
Clinical data
ATC code	none;
Identifiers
	IUPAC name 3-(4-(3-chlorophenyl)piperazin-1-yl)-1,1-diphenyl-2-propanol;
CAS Number	193611-72-2 ;
PubChem CID	3654103;
IUPHAR/BPS	10;
ChemSpider	2887678 ;
ChEMBL	ChEMBL534232 ;
CompTox Dashboard (EPA)	DTXSID4043983 ;
Chemical and physical data
Formula	C25H27ClN2O
Molar mass	406.95 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Clc2cccc(c2)N1CCN(CC1)CC(O)C(c3ccccc3)c4ccccc4;
	(what is this?) (verify)

BRL-15,572 is a drug which acts as a selective antagonist for the serotonin receptor subtype 5-HT_1D, with around 60x selectivity over other related receptors. The 5-HT_1D receptor has a very similar pharmacology to the closely related 5-HT_1B 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-HT_1D subtype while leaving 5-HT_1B 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-HT_1D 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

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. PMID 9303567.
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. PMID 9303568.
Marcoli M, Maura G, Munari C, Ruelle A, Raiteri M (February 1999). "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. doi:10.1038/sj.bjp.0702336. PMC 1565844. PMID 10188970.
Goadsby PJ, Classey JD (2003). "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. doi:10.1016/s0306-4522(03)00570-0. PMID 14614913.

This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.

[1] 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. PMID 9303567.

[2] 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. PMID 9303568.

[3] Marcoli M, Maura G, Munari C, Ruelle A, Raiteri M (February 1999). "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. doi:10.1038/sj.bjp.0702336. PMC 1565844. PMID 10188970.

[4] Goadsby PJ, Classey JD (2003). "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. doi:10.1016/s0306-4522(03)00570-0. PMID 14614913.