SKF-81,297
Clinical data
ATC code
  • none
Identifiers
  • 6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol
CAS Number
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC16H16ClNO2
Molar mass289.76 g·mol−1
3D model (JSmol)
  • Clc1c(O)c(O)cc2c1CCNCC2c3ccccc3

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

  1. ↑ Weed MR, Vanover KE, Woolverton WL (1993). "Reinforcing effect of the D1 dopamine agonist SKF 81297 in rhesus monkeys". Psychopharmacology. 113 (1): 51–2. doi:10.1007/BF02244333. PMID 7862828. S2CID 7292320.
  2. ↑ 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.
  3. ↑ Chausmer AL, Katz JL (January 2002). "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. doi:10.1007/s002130100896. PMID 11862342. S2CID 6788631.
  4. ↑ Graham DL, Hoppenot R, Hendryx A, Self DW (April 2007). "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. doi:10.1007/s00213-006-0473-5. PMID 16835769. S2CID 21192319.
  5. ↑ Delfino M, Kalisch R, Czisch M, Larramendy C, Ricatti J, Taravini IR, Trenkwalder C, Murer MG, Auer DP, Gershanik OS (September 2007). "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. doi:10.1038/sj.npp.1301329. PMID 17287822.
  6. ↑ Rashid AJ, So CH, Kong MM, et al. (2007). "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. Bibcode:2007PNAS..104..654R. doi:10.1073/pnas.0604049104. PMC 1766439. PMID 17194762.
  7. ↑ Akinori Nishi, et al. WO2012127871 (Kurume University, Nippon Medical School Foundation, Fujita Educational Inst, Rockefeller University).


This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.