75272-39-8

Colourless Crystalline Solid

A selective dopamine D2 receptor antagonist. Used as an antipsychotic

Nemonapride is a selective dopamine D2 receptor antagonist. Nemonapride is used as an antipsychotic.

Highly potent dopamine D 2 -like receptor antagonist; selective over D 1 -like receptors (K i values are 0.1 and 740 nM for D 2 -like and D 1 -like receptors respectively). Also potent 5-HT 1A receptor agonist (IC 50 = 34 nM) and has affinity for sigma receptors.

Nemonapride is a potent dopamine D₂receptor antagonist antipsychotic reported to have superior efficacy against hallucinations and delusions and also to be effective in the treatment of negative symptoms. The compound is a benzamide diastereomer and, although more potent than haloperidol, side effects are reported to be few primarily akinesia and some muscle rigidity with extrapyramidal symptoms being rare.

Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals. It binds dopamine 2 (D₂)-like receptors preferentially over D₁-like receptors (K_is = 0.06, 0.3, and 0.15 nM for D₂, D₃, and D₄, respectively). Nemonapride also binds sigma 1 (σ1) and σ2 receptors (K_is = 8.4 and 9.6 nM, respectively) and activates the serotonin 1A receptor (5-HT_1A; IC₅₀ = 34 nM).

Yamanouchi (Japan)

ChEBI: (2R,3R)-nemonapride is an optically active form of nemonapride having (2R,3R)-configuration. It is a conjugate base of a (2R,3R)-nemonapride(1+). It is an enantiomer of a (2S,3S)-nemonapride.

Emirace

Store at RT

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[2] RICHARD B MAILMAN  Xuemei H. Dopamine receptor pharmacology.[J]. Handbook of clinical neurology, 2007: 77-105. DOI: 10.1016/s0072-9752(07)83004-1
[3] H UJIKE  S K  K Akiyama. [3H]YM-09151-2 (nemonapride), a potent radioligand for both sigma 1 and sigma 2 receptor subtypes.[J]. Neuroreport, 1996, 7 5: 1057-1061. DOI: 10.1097/00001756-199604100-00021
[4] MARIE-BERNADETTE ASSIé  Wouter K  Cristina Cosi. 5-HT1A receptor agonist properties of the antipsychotic, nemonapride: comparison with bromerguride and clozapine[J]. European journal of pharmacology, 1997, 334 2: Pages 141-147. DOI: 10.1016/s0014-2999(97)01207-7