Pertine

Oxypertine, the most well-known drug of the pertine group.

The pertines, also known as phenylpiperazinylethylindoles, are a group of antipsychotics of the cyclized tryptamine and phenylpiperazine families that includes the following drugs:[1][2]

Oxypertine is known to show high affinity for the serotonin 5-HT2 and dopamine D2 receptors (Ki = 8.6 nM and 30 nM, respectively) and to also act as a catecholamine depleting agent.[2][3] Oxypertine, milipertine, and solypertine all antagonize the behavioral effects of tryptamine, a serotonin receptor agonist, and apomorphine, a dopamine receptor agonist, in animals.[2][4]

Some of the pertines, like milipertine and solypertine, are notable in containing an NBOMe-like moiety.[1][2]

The pertines were developed and initially described in the 1960s and 1970s.[1]

Chemical structures of pertines

See also

References

  1. ^ a b c Elks, J. (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. ISBN 978-1-4757-2085-3. Retrieved 18 June 2025.
  2. ^ a b c d Megens AA, Kennis LE (1996). "Risperidone and related 5HT2/D2 antagonists: a new type of antipsychotic agent?". Prog Med Chem. Progress in Medicinal Chemistry. 33: 185–232. doi:10.1016/s0079-6468(08)70306-0. ISBN 978-0-444-82310-6. PMID 8776944.
  3. ^ Bak IJ, Hassler R, Kim JS (1969). "Differential monoamine depletion by oxypertine in nerve terminals. Granulated synaptic vesicles in relation to depletion of norepinephrine, dopamine and serotonin". Zeitschrift für Zellforschung und Mikroskopische Anatomie. 101 (3): 448–462. doi:10.1007/BF00335580. PMID 5362847. S2CID 32583722.
  4. ^ Niemegeers CJ, Janssen PA (June 1979). "A systematic study of the pharmacological activities of dopamine antagonists". Life Sciences. 24 (24). Elsevier BV: 2201–2216. doi:10.1016/0024-3205(79)90096-1. PMID 388130.



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