Nemonapride is used in the treatment ofschizophrenia.[1][2] It is described as being effective in treating thepositive symptoms of schizophrenia.[1] It is also said to have someantidepressant andanxiolytic effects.[1] However, clinical data on nemonapride are described as being somewhat limited.[1]
In addition to the dopamineD2-like receptors, nemonapride has weaker affinity for theserotonin5-HT1A and5-HT2A receptors.[1] Its affinities (Ki) for these receptors are 1.8nM for the serotonin 5-HT1A receptor (11-fold lower than for the D2 receptor) and 9.4nM for the serotonin 5-HT2A receptor (59-fold lower than for the D2 receptor).[1] It is apartial agonist of the serotonin 5-HT1A receptor.[10][1][11] It has very weak affinity forsigma receptors (Ki = 80–3,000nM) as well.[12] Besides these specific receptors, nemonapride is described as having very weak affinity for the dopamineD1, serotonin5-HT2,adrenergic, andcholinergic receptors.[1]
Nemonapride is acis-2-methyl-3-amino-pyrrolidine derivative,[13] which was later shown to express most of its action as a drug to treatschizophrenia from itshomochiral (+)-(2R,3R) form.[14][15]
Nemonapride is thegeneric name of the drug and itsINNTooltip International Nonproprietary Name andJANTooltip Japanese Accepted Name.[8][7][19] It was also previously known asemonapride and by its former developmental code nameYM 09151-2.[8][7][19][20] In addition, nemonapride is known by its brand nameEmilace (JPTooltip Japanese language: エミレース) inJapan andChina.[8][7][19]
Nemonapride is marketed only inJapan andChina.[8][7] It was also under development for use in other countries, such asFrance, but development in other countries was discontinued.[3][1] There are no further plans for nemonapride to be developed for use in theUnited States, theUnited Kingdom, orEurope.[1]
^Newman-Tancredi A, Kleven MS (August 2011). "Comparative pharmacology of antipsychotics possessing combined dopamine D2 and serotonin 5-HT1A receptor properties".Psychopharmacology (Berl).216 (4):451–473.doi:10.1007/s00213-011-2247-y.PMID21394633.
^Assié MB, Cosi C, Koek W (September 1997). "5-HT1A receptor agonist properties of the antipsychotic, nemonapride: comparison with bromerguride and clozapine".Eur J Pharmacol.334 (2–3):141–147.doi:10.1016/s0014-2999(97)01207-7.PMID9369342.
^Wilson JM, Sanyal S, Van Tol HH (June 1998). "Dopamine D2 and D4 receptor ligands: relation to antipsychotic action".Eur J Pharmacol.351 (3):273–286.doi:10.1016/s0014-2999(98)00312-4.PMID9721018.
^abIwanami S, Takashima M, Hirata Y, Hasegawa O, Usuda S (October 1981). "Synthesis and neuroleptic activity of benzamides. Cis-N-(1-benzyl-2-methylpyrrolidin-3-yl)-5-chloro-2-methoxy-4-(methylamino)benzamide and related compounds".Journal of Medicinal Chemistry.24 (10). American Chemical Society (ACS):1224–1230.doi:10.1021/jm00142a019.PMID6120234.
^Harada S, Sakai T, Takasu K, Yamada K, Yamamoto Y, Tomioka K (September 2012). "General entry to asymmetric one-pot [N + 2 + n] cyclization for the synthesis of three- to seven-membered azacycloalkanes".The Journal of Organic Chemistry.77 (17). American Chemical Society (ACS):7212–7222.doi:10.1021/jo301495a.PMID22894619.
^Usuda S, Maeno H (January 1980). "Pharmacological Properties of a New Benzamide, YM-09151-2 With Potentially Neuroleptic Actions".Infolia Pharmacologica Japonica.76 (7). Japan: Japanese Pharmacological Soc.:184–185.
^Mori A, Kazamatsuri H, Kaneno S, Kamijima K, Kariya T, Murasaki M, et al. (1989). "A double-blind comparison of a new benzamide compound YM-09151 with haloperidol in the treatment of schizophrenia".Clin Eval.17:349–377.
^"-pride: sulpiride derivatives and analogues"(PDF).Use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. World Health Organization (WHO). 2024.
