UH-232
Encyclopedia
UH-232 is a drug which acts as a subtype selective mixed agonist-antagonist for dopamine receptor
s, acting as a weak partial agonist
at the D3
subtype, and an antagonist at D2Sh autoreceptor
s on dopaminergic nerve terminals. This causes dopamine release in the brain and has a stimulant
effect, as well as blocking the behavioural effects of cocaine. It was trialled for the treatment of schizophrenia but unexpectedly caused symptoms to become worse.
Dopamine receptor
Dopamine receptors are a class of metabotropic G protein-coupled receptors that are prominent in the vertebrate central nervous system . The neurotransmitter dopamine is the primary endogenous ligand for dopamine receptors....
s, acting as a weak 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...
at the D3
Dopamine receptor D3
D dopamine receptor is a protein that in humans is encoded by the DRD3 gene.This gene encodes the D3 subtype of the dopamine receptor. The D3 subtype inhibits adenylyl cyclase through inhibitory G-proteins. This receptor is expressed in phylogenetically older regions of the brain, suggesting that...
subtype, and an antagonist at D2Sh autoreceptor
Autoreceptor
An autoreceptor is a receptor located on presynaptic nerve cell membranes and serves as a part of a feedback loop in signal transduction. It is sensitive only to those neurotransmitters or hormones that are released by the neuron in whose membrane the autoreceptor sits.Canonically, a presynaptic...
s on dopaminergic nerve terminals. This causes dopamine release in the brain and has a stimulant
Stimulant
Stimulants are psychoactive drugs which induce temporary improvements in either mental or physical function or both. Examples of these kinds of effects may include enhanced alertness, wakefulness, and locomotion, among others...
effect, as well as blocking the behavioural effects of cocaine. It was trialled for the treatment of schizophrenia but unexpectedly caused symptoms to become worse.