Oxypertine Explained

Oxypertine, sold under the brand name Oxypertine among others, is an antipsychotic medication of the tryptamine and phenylpiperazine groups which was previously used in the treatment of schizophrenia but is no longer marketed.[1] It was also evaluated for the treatment of anxiety.[2]

Pharmacology

Pharmacodynamics

The drug shows high affinity for the serotonin 5-HT2 and dopamine D2 receptors (Ki = 8.6nM and 30nM, respectively).[3] It antagonizes the behavioral effects of tryptamine, a serotonin receptor agonist, and apomorphine, a dopamine receptor agonist, in animals.[4] Like reserpine and tetrabenazine, oxypertine depletes catecholamines, though not serotonin, possibly contributing to its antipsychotic effectiveness.[5]

Chemistry

Chemically, it is a substituted tryptamine and phenylpiperazine derivative.[6] Its chemical structure is similar to other "pertines" including alpertine, milipertine, and solypertine.[7] [8]

History

Oxypertine was first described in the scientific literature by 1962.

Society and culture

Names

Oxypertine is the generic name of the drug and its,,,, and .[9] [10] [11] [12] It is also known by its former developmental code name WIN-18501. The drug has been sold under brand names including Equipertine, Forit, Integrin, Lanturil, Lotawin, Opertil, and Oxypertine.

Notes and References

  1. Book: Dictionary of organic compounds . Chapman & Hall . London . 1996 . 0-412-54090-8 . Hall C, Rhodes PH .
  2. Somohano MD, Broissin MC, Sobrino ZA . [Clinical evaluation of oxypertine in anxiety conditions] . es . Neurologia, Neurocirugia, Psiquiatria . 17 . 3 . 171–180 . 1976 . 12484 .
  3. Megens AA, Kennis LE . Risperidone and related 5HT2/D2 antagonists: a new type of antipsychotic agent? . 33 . 185–232 . 1996 . 8776944 . 10.1016/s0079-6468(08)70306-0 . 978-0-444-82310-6 . Progress in Medicinal Chemistry .
  4. Niemegeers CJ, Janssen PA . A systematic study of the pharmacological activities of dopamine antagonists . Life Sciences . 24 . 24 . 2201–2216 . June 1979 . 388130 . 10.1016/0024-3205(79)90096-1 . Elsevier BV .
  5. Bak IJ, Hassler R, Kim JS . Differential monoamine depletion by oxypertine in nerve terminals. Granulated synaptic vesicles in relation to depletion of norepinephrine, dopamine and serotonin . Zeitschrift Fur Zellforschung und Mikroskopische Anatomie . 101 . 3 . 448–462 . 1969 . 5362847 . 10.1007/BF00335580 . 32583722 .
  6. Breulet M, Labar P, Delree C, Collard J, Bobon J . [Oxypertine, peperazine derivative of tryptophan with neuroleptic and dynamogenic properties] . fr . Acta Neurologica et Psychiatrica Belgica . 68 . 2 . 116–127 . February 1968 . 4972600 .
  7. Book: Ellis GP, Luscombe DK . Progress in Medicinal Chemistry . Elsevier Science . v. 33 . 1996 . 978-0-08-086281-1 . 30 October 2024 . 219 . Pertines (class 7; Table 5.12) The pertines oxypertine, solypertine, milipertine, and alpertine are piperazinylethylindoles..
  8. Book: Lednicer D, Mitscher LA . The Organic Chemistry of Drug Synthesis, Volume 2 . Wiley . Organic Chemistry Series of Drug Synthesis . 1980 . 978-0-471-04392-8 . 30 October 2024 . 341–343.
  9. Book: Elks J . The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies . Springer US . 2014 . 978-1-4757-2085-3 . 2 November 2024 . 924.
  10. Book: Schweizerischer Apotheker-Verein . Index Nominum 2000: International Drug Directory . Medpharm Scientific Publishers . 2000 . 978-3-88763-075-1 . 2 November 2024 . 779.
  11. Book: Morton IK, Hall JM . Concise Dictionary of Pharmacological Agents: Properties and Synonyms . Springer Netherlands . 2012 . 978-94-011-4439-1 . 2 November 2024 . 212.
  12. Web site: List of Antipsychotics . https://web.archive.org/web/20160303222344/https://drugs.com/international/oxypertine.html . 2016-03-03 .

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