BRL-15572
Izvor: Wikipedija
| |||
| (IUPAC) ime | |||
|---|---|---|---|
| 3-(4-(4-chlorophenyl)piperazin-1-yl)-1,1-diphenyl-2-propanol | |||
| Klinički podaci | |||
| Identifikatori | |||
| CAS broj | 193611-72-2 | ||
| ATC kod | nije dodeljen | ||
| PubChem[1][2] | 3654103 | ||
| ChEMBL[3] | CHEMBL534232 | ||
| Hemijski podaci | |||
| Formula | C25H27ClN2O | ||
| Mol. masa | 406.947 g/mol | ||
| SMILES | eMolekuli & PubHem | ||
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| Farmakoinformacioni podaci | |||
| Trudnoća | ? | ||
| Pravni status | |||
BRL-15,572 je lek koji deluje selektivni antagonist serotoninskog receptorskog tipa 5-HT1D, koji je oko 60x selektivniji u odnosu na srodne receptore.
5-HT1D receptor ima veoma sličnu farmakologiju sa blisko srodnim 5-HT1B receptorom, i većina starijih liganda tih receptora se vezuje za ova tipa sa aproksimativno jednakim afinitetom. Razvoj jedinjenja kao što je BRL-15572, koja imaju sposobnost selektivnog blokiranja 5-HT1D tipa, su znatno unapredila oruđa za istraživanje funkcije tog serotoninskog receptora.[4][5] Jedna od otkrivenih funkcija 5-HT1D receptora je njegova uloga u modulaciji otpuštanja neurotransmitera glutamata u mozgu,[6] kao i funkcije u regulaciji cerebralnog krvnog pritiska koje su važne u patogenezi migrenskih glavobolja.[7]
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.
- ↑ 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
- ↑ 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
- ↑ 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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