THIQ

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THIQ
(IUPAC) ime
N-[(3R)-1,2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl) -2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1ylmethyl)piperidin-1-yl]-2-oxoethylamine
Klinički podaci
Identifikatori
CAS broj 312637-48-2
ATC kod  ?
PubChem[1][2] 9938402
Hemijski podaci
Formula C33H41ClN6O2 
Mol. masa 589.169
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

THIQ je lek koji se koristi u naučnim istraživanjima. On je bio prvi nepeptidni agonist selektivan za melanokortinski receptor tip MC4.[3][4] U životinjskim studijama, je pokazano da THIQ stimuliše seksualnu aktivnost pacova,[5] i da ima neznatan uticaj na apetit ili inflamaciju.[6] To ide u podršku mogućoj primeni MC4 selektivnih agonista za treatman seksualne disfunkcije kod ljudi.[7] THIQ ima nedovolju bioraspoloživost i kratko vreme trajanja, tako da treba razviti poboljšane analoge.[8]

Vidi još[uredi - уреди]

Reference[uredi - уреди]

  1. 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.  edit
  2. 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. 
  3. Mutulis F, Yahorava S, Mutule I, Yahorau A, Liepinsh E, Kopantshuk S, Veiksina S, Tars K, Belyakov S, Mishnev A, Rinken A, Wikberg JE (August 2004). "New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ"". Journal of Medicinal Chemistry 47 (18): 4613–26. doi:10.1021/jm0311285. PMID 15317471. 
  4. Pogozheva ID, Chai BX, Lomize AL, Fong TM, Weinberg DH, Nargund RP, Mulholland MW, Gantz I, Mosberg HI (August 2005). "Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists". Biochemistry 44 (34): 11329–41. doi:10.1021/bi0501840. PMC 2532597. PMID 16114870. 
  5. Martin WJ, McGowan E, Cashen DE, Gantert LT, Drisko JE, Hom GJ, Nargund R, Sebhat I, Howard AD, Van der Ploeg LH, MacIntyre DE (November 2002). "Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula". European Journal of Pharmacology 454 (1): 71–9. doi:10.1016/S0014-2999(02)02479-2. PMID 12409007. 
  6. Muceniece R, Zvejniece L, Vilskersts R, Liepinsh E, Baumane L, Kalvinsh I, Wikberg JE, Dambrova M (December 2007). "Functional evaluation of THIQ, a melanocortin 4 receptor agonist, in models of food intake and inflammation". Basic & Clinical Pharmacology & Toxicology 101 (6): 416–20. doi:10.1111/j.1742-7843.2007.00133.x. PMID 18028105. 
  7. Shadiack AM, Sharma SD, Earle DC, Spana C, Hallam TJ (2007). "Melanocortins in the treatment of male and female sexual dysfunction". Current Topics in Medicinal Chemistry 7 (11): 1137–44. doi:10.2174/156802607780906681. PMID 17584134. 
  8. King SH, Mayorov AV, Balse-Srinivasan P, Hruby VJ, Vanderah TW, Wessells H (2007). "Melanocortin receptors, melanotropic peptides and penile erection". Current Topics in Medicinal Chemistry 7 (11): 1098–1106. PMC 2694735. PMID 17584130. 

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