SKF-81,297

SKF-81,297

SKF-81,297
Systematic (IUPAC) name
6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol
Clinical data
Legal status
?
Identifiers
CAS number
ATC code None
PubChem
ChemSpider
Chemical data
Formula C16H16ClNO2 
Mol. mass 289.76 g/mol

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]

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.  
  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.  
  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.  
  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.  
  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.  
  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.