타라나반트

Taranabant
타라나반트
Skeletal formula of taranabant
Space-filling model of the taranabant molecule
임상자료
경로:
행정		구강
ATC 코드
법적현황
법적현황
  • 조사(실패)
식별자
  • N-[(2S,3S)-4-(4-클로로페닐)-3-(3-시아노페닐)-2-부타닐]-2-메틸-2-{[5-(트리플루오로메틸)-2-피리디닐]옥시닐}프로파나미드
CAS 번호
펍켐 CID
켐스파이더
유니
CompTox 대시보드 (EPA)
ECHA InfoCard100.207.983 Edit this at Wikidata
화학 및 물리적 데이터
공식C27H25CLF3N3O2
어금질량515.96 g·190−1
3D 모델(JSmol)
  • C[C@H]([C@@H])(CC1=CC=C(C=C1)Cl)C2=CC(=C2)C#N)NC(=O)C(C)(C)OC3=NC=C(C=C3)C(F)(F)f
  • InChI=1S/C27H25ClF3N3O2/c1-17(34-25(35)26(2,3)36-24-12-9-21(16-33-24)27(29,30)31)23(14-18-7-10-22(28)11-8-18)20-6-4-5-19(13-20)15-32/h4-13,16-17,23H,14H2,1-3H3,(H,34,35)/t17-,23+/m0/s1
  • 키:QLYKJCMUNUWAGO-GAJHUEQPSA-N
(iii)

타라나반트(Codenamed MK-0364)는 식나비노이드 수용체 1형(1CB) 역작용제로, 식이노이드 효과가 있어 비만의 잠재적 치료제로 연구되었다.[1][2] 그것은 Merck & Co에 의해 발견되었다.

2008년 10월 머크는 주로 우울증과 불안감 등 중추신경계 부작용이 높아 이 약물로 임상3상을 중단했다.[3][4][5][6]

참고 항목

참조

  1. ^ Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, et al. (2007). "Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists". Bioorganic & Medicinal Chemistry Letters. 17 (8): 2184–7. doi:10.1016/j.bmcl.2007.01.087. PMID 17293109.
  2. ^ Fong TM, Guan XM, Marsh DJ, Shen CP, Stribling DS, Rosko KM, et al. (Jun 2007). "Antiobesity efficacy of a novel cannabinoid-1 receptor inverse agonist, N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-5-(trifluoromethyl)pyridin-2-yl]oxy]propanamide (MK-0364), in rodents". Journal of Pharmacology and Experimental Therapeutics. 321 (3): 1013–22. doi:10.1124/jpet.106.118737. PMID 17327489. S2CID 20001781.
  3. ^ "Press release by Merck". Retrieved 4 October 2008.
  4. ^ Aronne LJ, Tonstad S, Moreno M, Gantz I, Erondu N, Suryawanshi S, Molony C, Sieberts S, Nayee J, Meehan AG, Shapiro D, Heymsfield SB, Kaufman KD, Amatruda JM (May 2010). "A clinical trial assessing the safety and efficacy of taranabant, a CB1R inverse agonist, in obese and overweight patients: a high-dose study". International Journal of Obesity. 34 (5): 919–35. doi:10.1038/ijo.2010.21. PMID 20157323.
  5. ^ Kipnes MS, Hollander P, Fujioka K, Gantz I, Seck T, Erondu N, Shentu Y, Lu K, Suryawanshi S, Chou M, Johnson-Levonas AO, Heymsfield SB, Shapiro D, Kaufman KD, Amatruda JM (June 2010). "A one-year study to assess the safety and efficacy of the CB1R inverse agonist taranabant in overweight and obese patients with type 2 diabetes". Diabetes, Obesity & Metabolism. 12 (6): 517–31. doi:10.1111/j.1463-1326.2009.01188.x. PMID 20518807. S2CID 23886192.
  6. ^ Proietto J, Rissanen A, Harp JB, Erondu N, Yu Q, Suryawanshi S, Jones ME, Johnson-Levonas AO, Heymsfield SB, Kaufman KD, Amatruda JM (August 2010). "A clinical trial assessing the safety and efficacy of the CB1R inverse agonist taranabant in obese and overweight patients: low-dose study". International Journal of Obesity. 34 (8): 1243–54. doi:10.1038/ijo.2010.38. PMID 20212496.


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