NEMONAPRIDE

Description

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.

Description

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).

Chemical properties

Colourless Crystalline Solid

Originator

Yamanouchi (Japan)

The Uses of NEMONAPRIDE

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

The Uses of NEMONAPRIDE

A selective dopamine D2 receptor antagonist. Used as an antipsychotic

What are the applications of Application

Nemonapride is a dopamine D2 receptor (D2DR) antagonist

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.

brand name

Emirace

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.

Storage

Store at RT