Clocapramine (Clofekton, Padrasen), also known as 3-chlorocarpipramine, is an atypical antipsychotic of the iminostilbene class which was introduced in Japan in 1974 by Yoshitomi for the treatment of schizophrenia.[1][2][3][4][5] In addition to psychosis, clocapramine has also been used to augment antidepressants in the treatment of anxiety and panic.[6]
Clocapramine has been reported to act as an antagonist of the D2, 5-HT2A, α1-adrenergic, and α2-adrenergic receptors, and does not inhibit the reuptake of either serotonin or norepinephrine.[4][7][8][9][10] It has also been shown to have affinity for SIGMAR1.[11] Clocapramine's affinity for the 5-HT2A receptor is greater than that for the D2 receptor and it has a lower propensity for inducing extrapyramidal symptoms compared to typical antipsychotics, thus underlying its atypical nature.[4][5][10]
^David J. Triggle (1997). Dictionary of pharmacological agents. London: Chapman & Hall. ISBN 978-0-412-46630-4.
^Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. p. 1932. ISBN 978-3-88763-075-1.
^Sittig, Marshall (1988). Pharmaceutical manufacturing encyclopedia. Park Ridge, N.J., U.S.A: Noyes Publications. pp. 1756. ISBN 978-0-8155-1144-1. clocapramine.
^ abcSumiyoshi T, Suzuki K, Sakamoto H, et al. (February 1995). "Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy". Neuropsychopharmacology. 12 (1): 57–64. doi:10.1016/0893-133X(94)00064-7. PMID 7766287.
^ abOka T, Hamamura T, Lee Y, et al. (November 2004). "Atypical properties of several classes of antipsychotic drugs on the basis of differential induction of Fos-like immunoreactivity in the rat brain". Life Sciences. 76 (2): 225–37. doi:10.1016/j.lfs.2004.08.009. PMID 15519367.
^Saito M, Miyaoka H (August 2007). "Augmentation of paroxetine with clocapramine in panic disorder". Psychiatry and Clinical Neurosciences. 61 (4): 449. doi:10.1111/j.1440-1819.2007.01690.x. PMID 17610675. S2CID 38739899.
^Kurihara M, Tsumagari T, Setoguchi M, Fukuda T (1982). "A study on the pharmacological and biochemical profile of clocapramine". International Pharmacopsychiatry. 17 (2): 73–90. doi:10.1159/000468561. PMID 6125486.
^Tsukamoto T, Asakura M, Hirata N, Imafuku J, Matsui H, Hasegawa K (September 1984). "Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action". Biological Psychiatry. 19 (9): 1283–91. PMID 6149771.
^Setoguchi M, Sakamori M, Takehara S, Fukuda T (June 1985). "Effects of iminodibenzyl antipsychotic drugs on cerebral dopamine and alpha-adrenergic receptors". European Journal of Pharmacology. 112 (3): 313–22. doi:10.1016/0014-2999(85)90776-9. PMID 2862053.
^ abSchotte A, Bonaventure P, Janssen PF, Leysen JE (December 1995). "In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used". Japanese Journal of Pharmacology. 69 (4): 399–412. doi:10.1254/jjp.69.399. PMID 8786644.
^Morio Y, Tanimoto H, Yakushiji T, Morimoto Y (February 1994). "Characterization of the currents induced by sigma ligands in NCB20 neuroblastoma cells". Brain Research. 637 (1–2): 190–6. doi:10.1016/0006-8993(94)91232-7. PMID 7910100. S2CID 19250949.
Clocapramine (Clofekton, Padrasen), also known as 3-chlorocarpipramine, is an atypical antipsychotic of the iminostilbene class which was introduced in...
both tricyclics like imipramine and butyrophenones like haloperidol. Clocapramine Mosapramine Penfluridol (typical antipsychotic) Deniker P, Lôo H, Zarifian...
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