SKF-81,297 is a synthetic

drug A drug is any chemical substance other than a nutrient or an essential dietary ingredient, which, when administered to a living organism, produces a biological effect. Consumption of drugs can be via insufflation (medicine), inhalation, drug i ...

of the benzazepine

chemical class Chemical classification systems attempt to classify elements or compounds according to certain chemical functional or structural properties. Whereas the structural properties are largely intrinsic, functional properties and the derived classi ...

that acts as a selective dopamine D₁/ D₅ receptor full agonist, and produces a characteristic

stimulant Stimulants (also known as central nervous system stimulants, or psychostimulants, or colloquially as uppers) are a class of drugs that increase alertness. They are used for various purposes, such as enhancing attention, motivation, cognition, ...

-like pattern of anorexia,

hyperactivity Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by symptoms of inattention, hyperactivity, impulsivity, and emotional dysregulation that are excessive and pervasive, impairing in multiple ...

and

self-administration Self-administration is, in its Medicine, medical sense, the process of a subject administering a Pharmacology, pharmacological substance to themself. A clinical example of this is the subcutaneous "self-injection" of insulin by a Diabetes, diabetic ...

in animals. This profile is shared with several related drugs such as 6-Br-APB and SKF-82,958, but not with certain other D₁ full agonists such as A-77,636, reflecting

functional selectivity Functional selectivity (or agonist trafficking, biased agonism, biased signaling, ligand bias, and differential engagement) is the ligand-dependent selectivity for certain signal transduction pathways relative to a reference ligand (often the end ...

of D₁ activation. Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D₁-D₂ receptor heteromers. 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).

References

1-Phenyl-2,3,4,5-tetrahydro-1H-3-benzazepines Hydroxyarenes D1 receptor agonists D5 receptor agonists Chloroarenes {{gastrointestinal-drug-stub