Umespirone
Encyclopedia
Umespirone is a drug
of the azapirone class which possesses anxiolytic
and antipsychotic
properties. It behaves as a 5-HT1A receptor
partial agonist
(Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor
receptor antagonist
(Ki = 14 nM), and also has weak affinity for the sigma receptor
(Ki = 558 nM). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation
, cognitive/memory impairment
, catalepsy
, and extrapyramidal symptoms.
Drug
A drug, broadly speaking, is any substance that, when absorbed into the body of a living organism, alters normal bodily function. There is no single, precise definition, as there are different meanings in drug control law, government regulations, medicine, and colloquial usage.In pharmacology, a...
of the azapirone class which possesses anxiolytic
Anxiolytic
An anxiolytic is a drug used for the treatment of anxiety, and its related psychological and physical symptoms...
and antipsychotic
Antipsychotic
An antipsychotic is a tranquilizing psychiatric medication primarily used to manage psychosis , particularly in schizophrenia and bipolar disorder. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s...
properties. It behaves as a 5-HT1A receptor
5-HT1A receptor
The 5-HT1A receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin . It is a G protein-coupled receptor that is coupled to Gi/Go and mediates inhibitory neurotransmission...
partial agonist
Partial agonist
Partial agonists bind and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist...
(Ki = 15 nM), D2 receptor partial agonist (Ki = 23 nM), and α1-adrenoceptor
Alpha-1 adrenergic receptor
The alpha-1 adrenergic receptor is a G protein-coupled receptor associated with the Gq heterotrimeric G-protein. It consists of three highly homologous subtypes, including α1A-, α1B-, and α1D-adrenergic...
receptor antagonist
Receptor antagonist
A receptor antagonist is a type of receptor ligand or drug that does not provoke a biological response itself upon binding to a receptor, but blocks or dampens agonist-mediated responses...
(Ki = 14 nM), and also has weak affinity for the sigma receptor
Sigma receptor
The sigma receptors σ1 and σ2 bind to ligands such as 4-PPBP, SA 4503, ditolylguanidine, dimethyltryptamine and siramesine.- Classification :...
(Ki = 558 nM). Unlike many other anxiolytics and antipsychotics, umespirone produces minimal sedation
Sedation
Sedation is the reduction of irritability or agitation by administration of sedative drugs, generally to facilitate a medical procedure or diagnostic procedure...
, cognitive/memory impairment
Cognitive deficit
Cognitive deficit, also known as cognitive impairment is an inclusive term to describe any characteristic that acts as a barrier to cognitive performance...
, catalepsy
Catalepsy
Catalepsy is also a term used by hypnotists to refer to the state of making a hypnotised subject's arm, leg or back rigid. "Arm catalepsy" is often a pre-hypnotic test performed prior to an induction into a full trance.-Causes:...
, and extrapyramidal symptoms.