이비피나반트
Ibipinabant | |
| 임상 데이터 | |
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| ATC 코드 |
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| 식별자 | |
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| CAS 번호 | |
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| 켐스파이더 | |
| 유니 | |
| 케그 | |
| 첸블 | |
| CompTox 대시보드 (EPA ) | |
| ECHA 정보 카드 | 100.158.931 |
| 화학 및 물리 데이터 | |
| 공식 | C24H22클론2N4O2S |
| 몰 질량 | 501.427 g/120−1 |
| 3D 모델(JSmol) | |
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  (이게 뭐죠?) (표준) | |
이비피나반트(SLV319, BMS-646,256)는 과학 연구에 사용되는 약물로 강력하고 선택성이 높은1 CB [1]길항제 역할을 한다.비록 클래스로 바로 경쟁 상대 모두 지금 그다지 좋아하지 않게 문제를rimonabant으로 본 후 잠재적인 anorectics로ibipinabant 이제 실험실 연구에서 사용된다. 특히 구조 활성 상관 연구 감소한 것 animals,[2]에 비만의 치료를 위해 연구되었다, 강력한 식욕을 감퇴시키는 영향을 미친다.면사포 구름CB의1 [3][4][5]대항마.이비피나반트의 구조적 유사체인 SLV330은 기억, 인지 및 중독 행동 [6][7]조절과 관련된 동물 모델에서 활성화되는 것으로 보고되었다.이비피나반트의 원자 효율적인 합성이 [8]보고되었다.
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레퍼런스
- ^ Lange JH, Coolen HK, van Stuivenberg HH, Dijksman JA, Herremans AH, Ronken E, et al. (January 2004). "Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists". Journal of Medicinal Chemistry. 47 (3): 627–43. doi:10.1021/jm031019q. PMID 14736243.
- ^ Need AB, Davis RJ, Alexander-Chacko JT, Eastwood B, Chernet E, Phebus LA, et al. (January 2006). "The relationship of in vivo central CB1 receptor occupancy to changes in cortical monoamine release and feeding elicited by CB1 receptor antagonists in rats". Psychopharmacology. 184 (1): 26–35. doi:10.1007/s00213-005-0234-x. PMID 16328376. S2CID 23402768.
- ^ Lange JH, van Stuivenberg HH, Veerman W, Wals HC, Stork B, Coolen HK, et al. (November 2005). "Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity". Bioorganic & Medicinal Chemistry Letters. 15 (21): 4794–8. doi:10.1016/j.bmcl.2005.07.054. PMID 16140010.
- ^ Srivastava BK, Joharapurkar A, Raval S, Patel JZ, Soni R, Raval P, et al. (November 2007). "Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model". Journal of Medicinal Chemistry. 50 (24): 5951–66. doi:10.1021/jm061490u. PMID 17979261.
- ^ Srivastava BK, Soni R, Joharapurkar A, Sairam KV, Patel JZ, Goswami A, et al. (February 2008). "Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole". Bioorganic & Medicinal Chemistry Letters. 18 (3): 963–8. doi:10.1016/j.bmcl.2007.12.036. PMID 18207393.
- ^ de Bruin, NMWJ; Prickaerts, J; Lange, JHM; Akkerman, S; Andriambeloson, E; de Haan, M; Wijnen, J; van Drimmelen, M; Hissink, E; Heijink, L; Kruse, CG (2010). "SLV330, a cannabinoid CB1 receptor antagonist, ameliorates deficits in the T-maze, object recognition and Social Recognition Tasks in rodents". Neurobiology of Learning and Memory. 93 (4): 522–531. doi:10.1016/j.nlm.2010.01.010. PMID 20132903. S2CID 207261719.
- ^ de Bruin, NMWJ; Lange, JHM; Kruse, CG; Herremans, AH; Schoffelmeer, ANM; van Drimmelen, M; De Vries, TJ (2011). "SLV330, a cannabinoid CB1 receptor antagonist, attenuates ethanol and nicotine seeking and improves inhibitory response control in rats". Behavioural Brain Research. 217 (2): 408–415. doi:10.1016/j.bbr.2010.11.013. PMID 21074574. S2CID 205882042.
- ^ Lange, JHM; Sanders, HJ; van Rheenen, J (2011). "An expedient atom-efficient synthesis of the cannabinoid CB1 receptor inverse agonist ibipinabant". Tetrahedron Letters. 52 (12): 1303–1305. doi:10.1016/j.tetlet.2011.01.068. ISSN 0040-4039.
