:SKF-81,297

{{Short description|Synthetic drug, a stimulant}}

{{Drugbox

| IUPAC_name = 6-chloro-1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol

| image = Skf-81297.svg

| tradename =

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| routes_of_administration =

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| CAS_number_Ref = {{cascite|correct|CAS}}

| CAS_number = 253446-15-0

| UNII_Ref = {{fdacite|correct|FDA}}

| UNII = J494DH8JRC

| ATC_prefix = none

| ATC_suffix =

| PubChem = 16219952

| ChemSpiderID = 1181

| C=16 | H=16 | Cl=1 | N=1 | O=2

| smiles = 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.{{cite journal |vauthors=Weed MR, Vanover KE, Woolverton WL |title=Reinforcing effect of the D1 dopamine agonist SKF 81297 in rhesus monkeys |journal=Psychopharmacology |volume=113 |issue=1 |pages=51–2 |year=1993 |pmid=7862828 |doi= 10.1007/BF02244333|s2cid=7292320 }} This profile is shared with several related drugs such as 6-Br-APB and SKF-82,958,{{cite journal |vauthors=Weed MR, Paul IA, Dwoskin LP, Moore SE, Woolverton WL |title=The relationship between reinforcing effects and in vitro effects of D1 agonists in monkeys |journal=The Journal of Pharmacology and Experimental Therapeutics |volume=283 |issue=1 |pages=29–38 |date=October 1997 |pmid=9336305 }} but not with certain other D₁ full agonists such as A-77,636, reflecting functional selectivity of D₁ activation.{{cite journal |vauthors=Chausmer AL, Katz JL |title=Comparison of interactions of D1-like agonists, SKF 81297, SKF 82958 and A-77636, with cocaine: locomotor activity and drug discrimination studies in rodents |journal=Psychopharmacology |volume=159 |issue=2 |pages=145–53 |date=January 2002 |pmid=11862342 |doi=10.1007/s002130100896 |s2cid=6788631 |url=https://zenodo.org/record/1232629}}{{cite journal |vauthors=Graham DL, Hoppenot R, Hendryx A, Self DW |title=Differential ability of D1 and D2 dopamine receptor agonists to induce and modulate expression and reinstatement of cocaine place preference in rats |journal=Psychopharmacology |volume=191 |issue=3 |pages=719–30 |date=April 2007 |pmid=16835769 |doi=10.1007/s00213-006-0473-5 |s2cid=21192319 }}{{cite journal |vauthors=Delfino M, Kalisch R, Czisch M, Larramendy C, Ricatti J, Taravini IR, Trenkwalder C, Murer MG, Auer DP, Gershanik OS |title=Mapping the effects of three dopamine agonists with different dyskinetogenic potential and receptor selectivity using pharmacological functional magnetic resonance imaging |journal=Neuropsychopharmacology |volume=32 |issue=9 |pages=1911–21 |date=September 2007 |pmid=17287822 |doi=10.1038/sj.npp.1301329 |doi-access=free }} Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D₁-D₂ receptor heteromers.{{cite journal |vauthors=Rashid AJ, So CH, Kong MM, etal |title=D1-D2 dopamine receptor heterooligomers with unique pharmacology are coupled to rapid activation of Gq/11 in the striatum |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=104 |issue=2 |pages=654–9 |year=2007 |pmid=17194762 |pmc=1766439 |doi=10.1073/pnas.0604049104 |bibcode=2007PNAS..104..654R |doi-access=free }}

One of the patented uses for SKF-81,297 is as an augmentation agent when combined with an appropriate choice of an antidepressant.Akinori Nishi, et al. WO2012127871 (Kurume University, Nippon Medical School Foundation, Fujita Educational Inst, Rockefeller University).