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 diff ...
s, acting as a weak
partial agonist
In pharmacology, partial agonists are drugs that bind to and activate a given Receptor (biochemistry), receptor, but have only partial Intrinsic activity, efficacy at the receptor relative to a full agonist. They may also be considered Ligand (bio ...
at the
D3 subtype, and an antagonist at D
2Sh
autoreceptor
An autoreceptor is a type of Receptor (biochemistry), receptor located in the cell membrane, membranes of neuron, nerve cells. It serves as part of a negative feedback loop in signal transduction. It is only sensitive to the neurotransmitters or ...
s on dopaminergic nerve terminals. It causes dopamine release in the brain and has a
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, ...
effect, as well as blocking the behavioural effects of cocaine.
It may also serve as a
5-HT2A 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.
]
See also
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7-OH-DPAT
7-OH-DPAT is a synthetic compound that acts as a dopamine receptor agonist with reasonable selectivity for the D3 receptor subtype, and low affinity for serotonin receptors, unlike its structural isomer 8-OH-DPAT. 7-OH-DPAT is self-administer ...
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Amisulpride
Amisulpride, sold under the brand names Socian and Barhemsys, is a medication used in the treatment of schizophrenia, acute psychotic episodes, depression, and nausea and vomiting. It is specifically used at lower doses intravenously to prev ...
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DETQ
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RDS-127
RDS-127 is a drug which is used in scientific research. It acts as a D2-like receptor agonist and also has some serotonin and adrenergic agonist effects, as well as some anticholinergic action, and produces both anorectic and pro-sexual eff ...
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PNU-99,194
PNU-99,194(A) (or U-99,194(A)) is a drug which acts as a moderately selective D3 receptor antagonist with ~15-30-fold preference for D3 over the D2 subtype. Though it has substantially greater preference for D3 over D2, the latter receptor doe ...
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Rotigotine
Rotigotine, sold under the brand name Neupro among others, is a dopamine agonist of the non- ergoline class of medications indicated for the treatment of Parkinson's disease and restless legs syndrome. It is formulated as a once-daily transderm ...
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UH-301
(S)-UH-301 is a drug and research chemical widely used in scientific studies. It acts as a selective 5-HT1A receptor silent antagonist. It is structurally related to 8-OH-DPAT
8-OH-DPAT is a research chemical of the aminotetralin chemical cl ...
References
{{Dopaminergics
2-Aminotetralins
Dipropylamino compounds
Methoxyphenethylamines
Stimulants
Phenol ethers
Dopamine antagonists
Dopamine agonists