Ritanserin

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Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research.[1]

Research

Ritanserin was tested in clinical trials for schizophrenia[2] and migraine.[3]

Pharmacology

Ritanserin acts as a selective 5-HT2A (Ki = 0.45 nM) and 5-HT2C receptor (Ki = 0.71 nM) antagonist.[2][4] It has relatively low affinity for the H1, D2, α1-adrenergic, and α2-adrenergic receptors (39-, 77-, 107-, and 166-fold lower relative to 5-HT2A, respectively).[4] The affinity of ritanserin for the 5-HT1A receptor is than 1 µM.[4] In addition to its affinity for the 5-HT2A and 5-HT2C receptors, ritanserin also binds to and antagonizes the 5-HT1D, 5-HT2B, 5-HT5A, 5-HT6, and 5-HT7 receptors.[5]

The atypical antipsychotic risperidone was developed from ritanserin.[6]

See also

References

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