SKF-81,297
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SKF-81,297 is a synthetic
drug A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via insuffla ...
of the
benzazepine Benzazepines are heterocyclic chemical compounds consisting of a benzene ring fused to an azepine ring. Examples include: File:Benazepril structure.svg, Benazepril File:Fenoldopam.svg, Fenoldopam File:GSK-189,254.svg, GSK-189,254 File:Ivabradine ...
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 classificat ...
that acts as a selective dopamine D1/ D5 receptor
full agonist An agonist is a chemical that activates a receptor to produce a biological response. Receptors are cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an antagonist blocks the action of the ago ...
, and produces a characteristic
stimulant Stimulants (also often referred to as psychostimulants or colloquially as uppers) is an overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and inv ...
-like pattern of
anorexia Anorexia nervosa, often referred to simply as anorexia, is an eating disorder characterized by low weight, food restriction, body image disturbance, fear of gaining weight, and an overpowering desire to be thin. ''Anorexia'' is a term of Gre ...
,
hyperactivity Attention deficit hyperactivity disorder (ADHD) is a neurodevelopmental disorder characterised by excessive amounts of inattention, hyperactivity, and impulsivity that are pervasive, impairing in multiple contexts, and otherwise age-inapp ...
and self-administration in animals. This profile is shared with several related drugs such as
6-Br-APB 6-Br-APB is a synthetic compound that acts as a selective D1 agonist, with the (''R'')-enantiomer being a potent full agonist, while the (''S'') enantiomer retains its D1 selectivity but is a weak partial agonist. (''R'')-6-Br-APB and similar ...
and
SKF-82,958 SKF-82,958 is a synthetic compound of the benzazepine class that acts as a D1/ D5 receptor full agonist. SKF-82,958 and similar D1-like-selective full agonists like SKF-81,297 and 6-Br-APB produce characteristic anorectic effects, hyperactivity ...
, but not with certain other D1 full agonists such as
A-77,636 A-77636 is a synthetic drug which acts as a selective D1 receptor full agonist. It has nootropic, anorectic, rewarding and antiparkinsonian effects in animal studies, but its high potency and long duration of action causes D1 receptor downregula ...
, 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 referen ...
of D1 activation. Newer findings reveal that SKF-81,297 additionally acts as a partial agonist at D1-D2 receptor heteromers.


References

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