UH-232 ((+)-UH232) is a drug which acts as a subtype selective mixed agonist-antagonist for

dopamine receptor Dopamine receptors are a class of G protein-coupled receptors that are prominent in the vertebrate central nervous system (CNS). Dopamine receptors activate different effectors through not only G-protein coupling, but also signaling through diffe ...

s, acting as a weak

partial agonist In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonistic e ...

at the D₃ subtype, and an antagonist at D₂Sh

autoreceptor An autoreceptor is a type of receptor located in the membranes of nerve cells. It serves as part of a negative feedback loop in signal transduction. It is only sensitive to the neurotransmitters or hormones released by the neuron on which the aut ...

s on dopaminergic nerve terminals. This causes dopamine release in the brain and has a

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 ...

effect, as well as blocking the behavioural effects of cocaine. It may also serve as a 5-HT_2A receptor agonist, based on animal studies. It was investigated in clinical trials for the treatment of schizophrenia, but unexpectedly caused symptoms to become worse.

(+)-AJ76

The N-monopropyl derivative (+)-AJ76 is an active metabolite of UH-232 and has practically identical effects. ]

References

{{Dopaminergics Stimulants Phenol ethers Aminotetralins Dopamine antagonists Dopamine agonists

(+)-AJ76

See also

References