Chemistry:SKF-81,297
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Short description: Synthetic drug, a stimulant
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| Formula | C16H16ClNO2 |
| Molar mass | 289.76 g·mol−1 |
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SKF-81,297 is a synthetic drug of the benzazepine chemical class that acts as a selective dopamine D1/D5 receptor full agonist, and produces a characteristic stimulant-like pattern of anorexia, hyperactivity and self-administration in animals.[1] This profile is shared with several related drugs such as 6-Br-APB and SKF-82,958,[2] but not with certain other D1 full agonists such as A-77,636, reflecting functional selectivity of D1 activation.[3][4][5] Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D1-D2 receptor heteromers.[6]
One of the patented uses for SKF-81,297 is as an augmentation agent when combined with an appropriate choice of an antidepressant.[7]
References
- ↑ "Reinforcing effect of the D1 dopamine agonist SKF 81297 in rhesus monkeys". Psychopharmacology 113 (1): 51–2. 1993. doi:10.1007/BF02244333. PMID 7862828.
- ↑ "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. October 1997. PMID 9336305.
- ↑ "Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents". Psychopharmacology 159 (2): 145–53. January 2002. doi:10.1007/s002130100896. PMID 11862342. https://zenodo.org/record/1232629.
- ↑ "Differential ability of D1 and D2 dopamine receptor agonists to induce and modulate expression and reinstatement of cocaine place preference in rats". Psychopharmacology 191 (3): 719–30. April 2007. doi:10.1007/s00213-006-0473-5. PMID 16835769.
- ↑ "Mapping the effects of three dopamine agonists with different dyskinetogenic potential and receptor selectivity using pharmacological functional magnetic resonance imaging". Neuropsychopharmacology 32 (9): 1911–21. September 2007. doi:10.1038/sj.npp.1301329. PMID 17287822.
- ↑ "D1-D2 dopamine receptor heterooligomers with unique pharmacology are coupled to rapid activation of Gq/11 in the striatum". Proc. Natl. Acad. Sci. U.S.A. 104 (2): 654–9. 2007. doi:10.1073/pnas.0604049104. PMID 17194762. Bibcode: 2007PNAS..104..654R.
- ↑ Akinori Nishi, et al. WO2012127871 (Kurume University, Nippon Medical School Foundation, Fujita Educational Inst, Rockefeller University).
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