THIQ

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
Identifikatori
CAS broj	312637-48-2
PubChem	CID 9938402
Hemijski podaci
Formula	C33H41ClN6O2
Molarna masa	589.169
	SMILES N4Cc1ccccc1CC4C(=O)NC(Cc(cc2)ccc2Cl)C(=O)N5CCC(CC5)(Cn6ncnc6)C3CCCCC3; ;

THIQ je lek koji se koristi u naučnim istraživanjima. On je bio prvi nepeptidni agonist selektivan za melanokortinski receptor tip MC₄.^[1]^[2] U životinjskim studijama, je pokazano da THIQ stimuliše seksualnu aktivnost pacova,^[3] i da ima neznatan uticaj na apetit ili inflamaciju.^[4] To ide u podršku mogućoj primeni MC₄ selektivnih agonista za treatman seksualne disfunkcije kod ljudi.^[5] THIQ ima nedovolju bioraspoloživost i kratko vreme trajanja, tako da treba razviti poboljšane analoge.^[6]

Vidi još уреди

Reference уреди

^ Mutulis F, Yahorava S, Mutule I, Yahorau A, Liepinsh E, Kopantshuk S, Veiksina S, Tars K, Belyakov S, Mishnev A, Rinken A, Wikberg JE (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. PMID 15317471. doi:10.1021/jm0311285.
^ Pogozheva ID, Chai BX, Lomize AL, Fong TM, Weinberg DH, Nargund RP, Mulholland MW, Gantz I, Mosberg HI (2005). „Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists”. Biochemistry. 44 (34): 11329—41. PMC 2532597  . PMID 16114870. doi:10.1021/bi0501840.
^ Martin WJ, McGowan E, Cashen DE, Gantert LT, Drisko JE, Hom GJ, Nargund R, Sebhat I, Howard AD, Van der Ploeg LH, MacIntyre DE (2002). „Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula”. European Journal of Pharmacology. 454 (1): 71—9. PMID 12409007. doi:10.1016/S0014-2999(02)02479-2.
^ Muceniece R, Zvejniece L, Vilskersts R, Liepinsh E, Baumane L, Kalvinsh I, Wikberg JE, Dambrova M (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. PMID 18028105. doi:10.1111/j.1742-7843.2007.00133.x.
^ 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. PMID 17584134. doi:10.2174/156802607780906681.
^ 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.

Spoljašnje veze уреди

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[pmid15317471-1] Mutulis F, Yahorava S, Mutule I, Yahorau A, Liepinsh E, Kopantshuk S, Veiksina S, Tars K, Belyakov S, Mishnev A, Rinken A, Wikberg JE (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. PMID 15317471. doi:10.1021/jm0311285.

[pmid16114870-2] Pogozheva ID, Chai BX, Lomize AL, Fong TM, Weinberg DH, Nargund RP, Mulholland MW, Gantz I, Mosberg HI (2005). „Interactions of human melanocortin 4 receptor with nonpeptide and peptide agonists”. Biochemistry. 44 (34): 11329—41. PMC 2532597  . PMID 16114870. doi:10.1021/bi0501840.

[pmid12409007-3] Martin WJ, McGowan E, Cashen DE, Gantert LT, Drisko JE, Hom GJ, Nargund R, Sebhat I, Howard AD, Van der Ploeg LH, MacIntyre DE (2002). „Activation of melanocortin MC(4) receptors increases erectile activity in rats ex copula”. European Journal of Pharmacology. 454 (1): 71—9. PMID 12409007. doi:10.1016/S0014-2999(02)02479-2.

[pmid18028105-4] Muceniece R, Zvejniece L, Vilskersts R, Liepinsh E, Baumane L, Kalvinsh I, Wikberg JE, Dambrova M (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. PMID 18028105. doi:10.1111/j.1742-7843.2007.00133.x.

[pmid17584134-5] 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. PMID 17584134. doi:10.2174/156802607780906681.

[pmid17584130-6] 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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