Perospirone is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial... Dainippon Sumitomo Pharma developed perospirone in Japan in 2001 for the treatment of acute schizophrenia and bipolar mania as well as chronic schizophrenia.
- Mechanism
- Curator reviewed · 2 references
Antagonism at D2 receptors is believed to relieve the positive symptoms of schizophrenia such as delusions, hallucinations, and thought disorders. Perospirone targets the mesolimbic patway to reverse the overactivity of the dopaminergic signalling via D2 receptors. 5-HT2A antagonism is thought to allevaite the negative symptoms and cognitive impairments of schizophrenia. These receptors are Gi/Go coupled receptors that lead to decreased neurotransmitter release and neuronal inhibition when activated, thus play a role in dopamine release regulation. Perospirone targets these receptors in the nigrostriatal pathway to reduce dopamine release and function. In contrast, 5-HT2A receptor antagonism may improve the negative symptoms by enhancing dopamine and glutamate release in the mesocortical pathway. 5-HT1A receptor activation further inhibits the release of 5-HT into the synaptic cleft.
- Primary indication
- For the treatment of schizophrenia and acute cases of bipolar mania.Curator reviewed
- Formula / weight
- C23H30N4O2S · 426.58 g/mol (avg)
- Also known as
- SM-9018
Resolves to
FBVFZWUMDDXLLG-HDICACEKSA-NSMILES[H][C@@]12CCCC[C@]1([H])C(=O)N(CCCCN1CCN(CC1)C1=NSC3=CC=CC=C13)C2=OWhat you can answer from here — as of March 06, 2025
Which drugs share a target with Perospirone, and which of those have an active Phase 3 trial?
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