SKF-82,958

SKF-82,958
SKF-82,958
SKF 82958.png
식별자
  • 3-알릴-6-클로로-1-페닐-1,2,4,5-테트라히드로-3-벤자제핀-7,8-디올
CAS 번호
PubChem CID
켐스파이더
유니
첸블
CompTox 대시보드 (EPA )
화학 및 물리 데이터
공식C19H20클론NO2
몰 질량329.82 g/120−1
3D 모델(JSmol)
  • C=CCN1CC2=C(=C(C=C2C(C1)C3=CC=CC=C3)O)O)클론

SKF-82,958은 D/D5 수용체1 완전작용제 [1][2]역할을 하는 벤자제핀계 합성화합물이다.SKF-82,958 및 SKF-81,297 및 6-Br-APB와 같은 유사한 D-like-selective1 완전작용제는 동물에서 특징적인 식욕부진 효과, 과잉활동 및 자가투여를 발생시키며,[3][4][5][6][7][8][9][10][11] 암페타민과 같은 도파민성 자극제와 유사하지만 동일하지는 않다.SKF-82,958은 이후 ERβ에서 무시할 수 있는 활성으로 ERα의 작용제로 작용하여 아형 선택성 [12][13]에스트로겐이 되었다.

레퍼런스

  1. ^ Pfeiffer, Francis R.; Wilson, James W.; Weinstock, Joseph; Kuo, George Y.; Chambers, Pamela A.; Holden, Kenneth G.; Hahn, Richard A.; Wardell, Joseph R., Jr.; Alfonso, J. Tobia; et al. (1982). "Dopaminergic activity of substituted 6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines". Journal of Medicinal Chemistry. 25 (4): 352–358. doi:10.1021/jm00346a005. PMID 7069713.{{cite journal}}: CS1 maint: 여러 이름: 작성자 목록(링크)
  2. ^ Wang JQ, McGinty JF (May 1997). "The full D1 dopamine receptor agonist SKF-82958 induces neuropeptide mRNA in the normosensitive striatum of rats: regulation of D1/D2 interactions by muscarinic receptors". The Journal of Pharmacology and Experimental Therapeutics. 281 (2): 972–82. PMID 9152408.
  3. ^ Terry P, Katz JL (1992). "Differential antagonism of the effects of dopamine D1-receptor agonists on feeding behavior in the rat". Psychopharmacology. 109 (4): 403–9. doi:10.1007/BF02247715. PMID 1365854. S2CID 12871227.
  4. ^ Self DW, Stein L (June 1992). "The D1 agonists SKF 82958 and SKF 77434 are self-administered by rats". Brain Research. 582 (2): 349–52. doi:10.1016/0006-8993(92)90155-3. PMID 1356585. S2CID 9410802.
  5. ^ Rosenzweig-Lipson S, Hesterberg P, Bergman J (September 1994). "Observational studies of dopamine D1 and D2 agonists in squirrel monkeys". Psychopharmacology. 116 (1): 9–18. doi:10.1007/BF02244865. PMID 7862937. S2CID 24204026.
  6. ^ Kalivas PW, Duffy P (July 1995). "D1 receptors modulate glutamate transmission in the ventral tegmental area". Journal of Neuroscience. 15 (7 Pt 2): 5379–88. doi:10.1523/JNEUROSCI.15-07-05379.1995. PMC 6577867. PMID 7623160.
  7. ^ Weed MR, Woolverton WL (December 1995). "The reinforcing effects of dopamine D1 receptor agonists in rhesus monkeys". The Journal of Pharmacology and Experimental Therapeutics. 275 (3): 1367–74. PMID 8531104.
  8. ^ Weed MR, Paul IA, Dwoskin LP, Moore SE, Woolverton WL (October 1997). "The relationship between reinforcing effects and in vitro effects of D1 agonists in monkeys". The Journal of Pharmacology and Experimental Therapeutics. 283 (1): 29–38. PMID 9336305.
  9. ^ Abrahams BS, Rutherford JD, Mallet PE, Beninger RJ (February 1998). "Place conditioning with the dopamine D1-like receptor agonist SKF 82958 but not SKF 81297 or SKF 77434". European Journal of Pharmacology. 343 (2–3): 111–8. doi:10.1016/S0014-2999(97)01531-8. PMID 9570457.
  10. ^ Tidey JW, Bergman J (June 1998). "Drug discrimination in methamphetamine-trained monkeys: agonist and antagonist effects of dopaminergic drugs". The Journal of Pharmacology and Experimental Therapeutics. 285 (3): 1163–74. PMID 9618419.
  11. ^ Berridge KC, Aldridge JW (September 2000). "Super-stereotypy I: enhancement of a complex movement sequence by systemic dopamine D1 agonists" (PDF). Synapse. 37 (3): 194–204. doi:10.1002/1098-2396(20000901)37:3<194::AID-SYN3>3.0.CO;2-A. hdl:2027.42/34987. PMID 10881041.
  12. ^ Walters MR, Dutertre M, Smith CL (2002). "SKF-82958 is a subtype-selective estrogen receptor-alpha (ERalpha ) agonist that induces functional interactions between ERalpha and AP-1". J. Biol. Chem. 277 (3): 1669–79. doi:10.1074/jbc.M109320200. PMID 11700319.
  13. ^ Adam Gideon King (2002). Estrogen induces uterine angiogenesis through the expression of vascular endothelial growth factor. University of Wisconsin--Madison. p. 21.


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