niaprazine

Niaprazine is a sedative-hypnotic drug of the phenylpiperazine class, primarily used for the short-term management of insomnia and sleep disturbances, especially in children. It was initially believed to act as an antihistamine and anticholinergic but was later found to have low or no affinity for histamine H1 and muscarinic acetylcholine receptors. Instead, its primary mechanism is potent and selective antagonism at serotonin 5-HT2A receptors (Ki ≈ 25 nM) and alpha-1 adrenergic receptors (Ki ≈ 77–86 nM). Niaprazine has little or no affinity for dopamine D2, beta-adrenergic, serotonin transporter (SERT), vesicular monoamine transporter (VMAT), or other serotonergic receptor subtypes. It also acts as a selective brain catecholamine depletor. The drug has been marketed since the early 1970s in several European countries under the brand name Nopron[1][2][4][5][6]. Niaprazine is metabolized to para-fluorophenylpiperazine (pFPP), though this metabolite does not contribute to its sedative effects[1]. It has also been investigated for use in sleep disorders associated with attention-deficit hyperactivity disorder and autistic disorder[5][7].

Brand names

Nopron

Other names

niaprazinaniaprazinum