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| Other names | SKF81297; SKF-81297; SK&F-81297; SK&F-81,297; SK&F81297 |
| Routes of administration | Oral[1] |
| Drug class | Dopamine receptor agonist;DopamineD1-like receptoragonist;Stimulant;Antiparkinsonian agent |
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| Chemical and physical data | |
| Formula | C16H16ClNO2 |
| Molar mass | 289.76 g·mol−1 |
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SKF-81,297 is adopamineD1-like receptoragonist andstimulant-likedrug of the3-benzazepine family which was under development for the treatment ofParkinson's disease but was never marketed.[1][2][3] It is acyclized phenethylamine andcatecholamine and is amodifiedderivative of themonoamine neurotransmitterdopamine.[4] The drug is takenorally.[1]
The drug acts as aselective dopamineD1 andD5 receptorfull agonist.[3] In addition, it acts as apartial agonist at dopamineD1–D2 receptor heteromers.[5] It produces a characteristic stimulant-like pattern of effects includinganorexia,hyperactivity, andself-administration in animals.[3] This profile is shared with several related drugs such as6-Br-APB andSKF-82,958,[6] but not with certain other dopamine D1 receptor full agonists such asA-77,636, reflectingfunctional selectivity of dopamine D1 receptor activation.[7][8][9] The drug also producespro-motivational effects in animals.[10]
Although it produces stimulant-like effects in animals, SKF-81,297 did not substitute fordextroamphetamine in rodentdrug discrimination tests in multiple studies.[11][12] This is in notable contrast to dopamineD2 receptor agonists likequinpirole andRU-24213, which fully substitute for dextroamphetamine in such tests.[13] However, in another study, higher doses of SKF-81,297 were able to partially substitute for dextroamphetamine.[13]
SKF-81,297 readily crosses theblood–brain barrier in rodents and shows substantially greaterpenetration than the related dopamine D1-like receptor agonistSKF-38,393.[12] Its predictedlog P is 2.7.[14]
SKF-81,297 was first described in thescientific literature by 1988.[15] It was developed byGlaxoSmithKline.[1][2] The drug reached thepreclinical research stage of development for Parkinson's disease prior to the discontinuation of its development.[1][2] One of thepatented uses for SKF-81,297 is as anaugmentation agent when combined with an appropriate choice of anantidepressant.[16]
