Chemistry:Sonepiprazole
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| Routes of administration | Oral |
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| Formula | C21H27N3O3S |
| Molar mass | 401.53 g·mol−1 |
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Sonepiprazole (U-101,387, PNU-101,387-G) is a drug of the phenylpiperazine class which acts as a highly selective D4 receptor antagonist.[1] In animals, unlike D2 receptor antagonists like haloperidol, sonepiprazole does not block the behavioral effects of amphetamine or apomorphine, does not alter spontaneous locomotor activity on its own, and lacks extrapyramidal and neuroendocrine effects.[2] However, it does reverse the prepulse inhibition deficits induced by apomorphine,[3] and has also been shown to enhance cortical activity and inhibit stress-induced cognitive impairment.[4][5] As a result, it was investigated as an antipsychotic for the treatment of schizophrenia in a placebo-controlled clinical trial, but in contrast to its comparator olanzapine no benefits were found and it was not researched further for this indication.[6][7]
See also
- Phenylpiperazine
- PNU-142633
- Terikalant
References
- ↑ "(S)-(−)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist". Journal of Medicinal Chemistry 39 (13): 2435–7. June 1996. doi:10.1021/jm960084f. PMID 8691438.
- ↑ "Pharmacological characterization of U-101387, a dopamine D4 receptor selective antagonist". The Journal of Pharmacology and Experimental Therapeutics 279 (3): 1392–403. December 1996. PMID 8968364. http://jpet.aspetjournals.org/cgi/pmidlookup?view=long&pmid=8968364.
- ↑ "Selective dopamine D4 receptor antagonists reverse apomorphine-induced blockade of prepulse inhibition". Psychopharmacology 135 (2): 194–200. January 1998. doi:10.1007/s002130050501. PMID 9497025. http://link.springer.de/link/service/journals/00213/bibs/8135002/81350194.htm.
- ↑ "Dopamine D4 receptor-deficient mice display cortical hyperexcitability". Journal of Neuroscience 21 (11): 3756–63. June 2001. doi:10.1523/JNEUROSCI.21-11-03756.2001. PMID 11356863.
- ↑ "The selective dopamine D4 receptor antagonist, PNU-101387G, prevents stress-induced cognitive deficits in monkeys". Neuropsychopharmacology 23 (4): 405–10. October 2000. doi:10.1016/S0893-133X(00)00133-0. PMID 10989267.
- ↑ "Chromeno[3,4-c]pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents". Journal of Medicinal Chemistry 40 (17): 2688–93. August 1997. doi:10.1021/jm970170v. PMID 9276014.
- ↑ "Effectiveness of the selective D4 antagonist sonepiprazole in schizophrenia: a placebo-controlled trial". Biological Psychiatry 55 (5): 445–51. March 2004. doi:10.1016/j.biopsych.2003.10.004. PMID 15023570.
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