Pirenperone (, , ; developmental code names R-47456, R-50656) is a

serotonin receptor antagonist A serotonin antagonist, or serotonin receptor antagonist, is a drug used to inhibit the action of serotonin and serotonergic drugs at serotonin receptor, serotonin (5-HT) receptors. Types 5-HT2A antagonists Antagonists of the 5-HT2A, 5-HT2A re ...

closely related to

ketanserin Ketanserin, sold under the brand name Sufrexal, is an antihypertensive agent which is used to treat arterial hypertension and vasospasm, vasospastic disorders. It is also used in scientific research as an antiserotonergic medication, agent in th ...

and

risperidone Risperidone, sold under the brand name Risperdal among others, is an atypical antipsychotic used to treat schizophrenia and bipolar disorder, as well as aggressive and self-injurious behaviors associated with autism spectrum disorder. It is t ...

which is described as an

antipsychotic Antipsychotics, previously known as neuroleptics and major tranquilizers, are a class of Psychiatric medication, psychotropic medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), p ...

and

tranquilizer A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are central nervous system (CNS) depressants and interact with brain activity, causing its deceleration. Various kinds of sedatives c ...

and was never marketed. It is a relatively selective

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

5-HT_2A receptor and has been used in

scientific research The scientific method is an empirical method for acquiring knowledge that has been referred to while doing science since at least the 17th century. Historically, it was developed through the centuries from the ancient and medieval world. The ...

to study the

serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

system. Its affinities (K_i) for serotonin and other receptors have been reported to be 0.3 to 1.1nM for the serotonin 5-HT_2A receptor, 6.5nM for the serotonin 5-HT₇ receptor, 20nM for the α_1B-adrenergic receptor, 20nM for the α_2B-adrenergic receptor, 61nM for the serotonin 5-HT_2B receptor, 60 to 77nM for the serotonin 5-HT_2C receptor, 485 to 1,700nM for the serotonin 5-HT_1A receptor, and >1,000 or 6,600nM for the serotonin 5-HT_1B receptor, whereas other receptors were not reported. In the 1980s, the drug was found to block the effects of the

lysergic acid diethylamide Lysergic acid diethylamide, commonly known as LSD (from German ; often referred to as acid or lucy), is a Semisynthesis, semisynthetic, Hallucinogen, hallucinogenic compound derived from ergot, known for its powerful psychological effects and ...

(LSD) in animals, and, along with

, led to the elucidation of the 5-HT_2A receptor as the biological mediator of the effects of serotonergic psychedelics.

References

{{Serotonin receptor modulators 5-HT2 antagonists Abandoned drugs Antipsychotics Anxiolytics 4-Fluorophenyl compounds Ketones Piperidines Pyridopyrimidines

See also

References