HOME

TheInfoList



OR:

SKF-81,297 is a
synthetic Synthetic may refer to: Science * Synthetic biology * Synthetic chemical or compound, produced by the process of chemical synthesis * Synthetic elements, chemical elements that are not naturally found on Earth and therefore have to be created in ...
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 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 agoni ...
, 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 Anorexia nervosa (AN), often referred to simply as anorexia, is an eating disorder characterized by Calorie restriction, food restriction, body image disturbance, fear of gaining weight, and an overpowering desire to be thin. Individuals wit ...
,
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 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, hyperac ...
, 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 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