Description
Nemonapride is a potent dopamine D
2receptor 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.
Description
Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals. It binds dopamine 2 (D
2)-like receptors preferentially over D
1-like receptors (K
is = 0.06, 0.3, and 0.15 nM for D
2, D
3, and D
4, 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; IC
50 = 34 nM).
Chemical Properties
Colourless Crystalline Solid
Originator
Yamanouchi (Japan)
Uses
Nemonapride is a selective dopamine D2 receptor antagonist. Nemonapride is used as an antipsychotic.
Uses
A selective dopamine D2 receptor antagonist. Used as an antipsychotic
Definition
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.
Biological Activity
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.
References
[1] MICHLO TERAI . SELECTIVE BINDING OF YM-09151-2, A NEW POTENT NEUROLEPTIC, TO D2-DOPAMINERGIC RECEPTORS[J]. Japanese journal of pharmacology, 1983, 33 4: Pages 749-755. DOI:
10.1016/s0021-5198(19)52463-5[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
