SKF-82,958
SKF-82,958
Chemical compound
SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/D5 receptor full agonist.[1][2] SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulants such as amphetamine.[3][4][5][6][7][8][9][10][11] SKF-82,958 was also subsequently found to act as an agonist of ERα with negligible activity at ERβ, making it a subtype-selective estrogen.[12][13]
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Formula | C19H20ClNO2 |
Molar mass | 329.82 g·mol−1 |
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- Pfeiffer FR, Wilson JW, Weinstock J, Kuo GY, Chambers PA, Holden KG, et al. (April 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.
- 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): 972–982. PMID 9152408.
- Terry P, Katz JL (1992). "Differential antagonism of the effects of dopamine D1-receptor agonists on feeding behavior in the rat". Psychopharmacology. 109 (4): 403–409. doi:10.1007/BF02247715. PMID 1365854. S2CID 12871227.
- Kalivas PW, Duffy P (July 1995). "D1 receptors modulate glutamate transmission in the ventral tegmental area". The Journal of Neuroscience. 15 (7 Pt 2): 5379–5388. doi:10.1523/JNEUROSCI.15-07-05379.1995. PMC 6577867. PMID 7623160.
- 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): 111–118. doi:10.1016/S0014-2999(97)01531-8. PMID 9570457.
- Berridge KC, Aldridge JW (September 2000). "Super-stereotypy I: enhancement of a complex movement sequence by systemic dopamine D1 agonists". 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. S2CID 13215977.
- Walters MR, Dutertre M, Smith CL (January 2002). "SKF-82958 is a subtype-selective estrogen receptor-alpha (ERalpha ) agonist that induces functional interactions between ERalpha and AP-1". The Journal of Biological Chemistry. 277 (3): 1669–1679. doi:10.1074/jbc.M109320200. PMID 11700319.
- King AG (2002). Estrogen induces uterine angiogenesis through the expression of vascular endothelial growth factor (Ph.D. thesis). University of Wisconsin--Madison. p. 21.
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