Niaprazine
(Synonyms: 尼普拉嗪) 目录号 : GC61467
Niaprazine是一种具有强效镇静作用的组胺H1受体(histamineH1-receptor)拮抗剂。Niaprazine具有抗组胺和抗血清素活性，并可用于睡眠障碍的研究。
Cas No.:27367-90-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research[1][2].
Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, α2, β, H1 and mAch receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for α1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites[2].
Niaprazine (60 mg/kg; i.p.; once) treatment increases rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Niaprazine also produces a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA)[3]. Animal Model: Male Sprague-Dawley rats (150-200 g)[3]
[1]. D Scherman, et al. Molecular pharmacology of niaprazine. Prog Neuropsychopharmacol Biol Psychiatry. 1988;12(6):989-1001. [2]. P G Rossi, et al. Niaprazine in the treatment of autistic disorder. J Child Neurol. 1999 Aug;14(8):547-50. [3]. P E Keane, et al. The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain. Neuropharmacology. 1982 Feb;21(2):163-9.
| Cas No. | 27367-90-4 | SDF | |
| 别名 | 尼普拉嗪 | ||
| Canonical SMILES | O=C(C1=CN=CC=C1)NC(C)CCN2CCN(C3=CC=C(F)C=C3)CC2 | ||
| 分子式 | C20H25FN4O | 分子量 | 356.44 |
| 溶解度 | DMSO: 100 mg/mL (280.55 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8055 mL | 14.0276 mL | 28.0552 mL |
| 5 mM | 0.5611 mL | 2.8055 mL | 5.611 mL |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8055 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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1. 首先保证母液是澄清的；
2.
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Niaprazine in the treatment of autistic disorder
J Child Neurol 1999 Aug;14(8):547-50.PMID:10456769DOI:10.1177/088307389901400814.
Niaprazine is a histamine H1-receptor antagonist with marked sedative properties. It has been employed in subjects with behavior and sleep disorders. No data concerning the use of Niaprazine in subjects with autistic disorder are reported in the literature. The authors performed an open study to assess Niaprazine efficacy in a sample of 25 subjects with autistic disorder and associated behavior and sleep disorders. Niaprazine was administered at 1 mg/kg/day for 60 days. A positive effect was found in 52% of patients, particularly on hyperkinesia, unstable attention, resistance to change and frustration, mild anxiety signs, heteroaggressiveness, and sleep disorders. Statistical comparison between responders and nonresponders showed no influence on Niaprazine effect by age over or under 12 years, presence of neurologic signs, epilepsy, or abnormalities seen on brain imaging. Niaprazine was more efficacious in subjects with a mild or moderate degree of mental retardation. No side effects were observed. Because of its sedative effects and good tolerability, Niaprazine can be used as a first-choice drug to improve behavior and sleep disorders in patients with autistic disorder.
Molecular pharmacology of Niaprazine
Prog Neuropsychopharmacol Biol Psychiatry 1988;12(6):989-1001.PMID:2853885DOI:10.1016/0278-5846(88)90093-0.
1. The pharmacological profile of Niaprazine was investigated using in vitro ligand binding techniques. 2. Niaprazine exhibits a low affinity for the vesicular monoamine transporter and for D2, alpha 2, beta, H1 and muscarinic cholinergic receptors. Niaprazine, particularly the (+)stereoisomer, has a higher affinity for alpha 1 (Ki = 77 nM) and 5-HT2 (Ki = 25 nM) binding sites, but is poorly recognized by 5-HT1A and 5-HT1B binding sites (Ki sigma mciroM). In contrast, p-fluoro-phenylpiperazine, a major metabolite of Niaprazine, exhibits a higher affinity for the 5-HT1 subclasses than for the 5HT2 class. 3. These results suggest that the pharmacological properties of Niaprazine reflect both its non-reserpinic catecholamine depletor effect and its action on alpha 1 and 5-HT2 receptors. A role of p-fluoro-phenylpiperazine via 5-HT1 sites cannot be excluded.
The effect of Niaprazine on the turnover of 5-hydroxytryptamine in the rat brain
Neuropharmacology 1982 Feb;21(2):163-9.PMID:6460945DOI:10.1016/0028-3908(82)90157-5.
Niaprazine (60 mg/kg i.p.) increased rat brain 5-hydroxyindole acetic acid (5-HIAA) concentrations 30 min after treatment, and reduced them at 3-8 hr after treatment. Rat brain 5-hydroxytryptamine (5-HT) levels were unchanged. Niaprazine also produced a short-lasting depletion of rat brain noradrenaline (NA) and dopamine (DA). Pretreatment with alpha-phenyl-alpha-propyl-benzeneacetic acid, 2-(diethylamino) ethyl ester hydrochloride (SKF 525A) (75 mg/kg i.p.) potentiated the increase in 5-HIAA and depletion of catecholamines produced 1 hr after Niaprazine, but abolished the reduction in 5-HIAA produced 8 hr after the drug. This suggested that a metabolite might be responsible for the delayed reduction in 5-HIAA levels. A potential metabolite, p-fluoro-phenylpiperazine (FPP) (5-40 mg/kg i.p.) reduced rat brain 5-HIAA and 3,4-dihydroxyphenyl acetic acid (DOPAC), and inhibited 5-HT and NA uptake in vitro. Unlike Niaprazine, FPP produced no behavioural sedation, but in large doses produced a behavioural syndrome indicative of serotonergic stimulation. Studies of the metabolism of 14C-niaprazine in rats indicated the presence of a urinary metabolite with the same chromatographic characteristics as FPP. These results suggest that Niaprazine itself depletes brain catecholamines and increases 5-HT turnover, while a metabolite, FPP, subsequently reduces the turnover of 5-HT and DA.
The effect of Niaprazine on some common sleep disorders in children. A double-blind clinical trial by means of continuous home-videorecorded sleep
Childs Nerv Syst 1991 Oct;7(6):332-5.PMID:1837245DOI:10.1007/BF00304832.
A placebo-controlled double-blind clinical trial on the effect of Niaprazine on children with some common sleep disorders was carried out. Niaprazine at a daily dosage of 1 mg/kg body weight or placebo at random was administered to a selected group of 36 children (aged from 6 months to 6 years) suffering from frequent nighttime waking or inability to fall asleep. The effect of Niaprazine (or placebo) on sleep disorders was studied by means of continuous home-videorecorded sleep before and after the trial. A reliable positive effect of Niaprazine on the sleep disorders considered was found. No adverse side effects were observed. We conclude that Niaprazine seems to represent an effective and safe drug for the therapy of frequent nighttime waking and inability to fall asleep.
[Niaprazine in behavior disorders in children. Double-blind comparison with placebo]
Pediatr Med Chir 1987 Mar-Apr;9(2):185-7.PMID:2958783doi
The results of a randomized, double blind clinical trial are described. Niaprazine (1.5 mg/kg/day) or placebo were administered for 1 month to 20 patients (17 M-3 F; age range 6-11 years) suffering from behaviour disorders. Both the active drug and placebo induced an improvement of behaviour in the various conditions assessed in the family, during the play, at school, in the doctor's office but the percent variation induced by Niaprazine was always higher than that with placebo (mean -49.4% vs. -24.6). The difference between the treatments was highly significant. No relevant side effects were observed: only in two cases treated with Niaprazine the daily dose was reduced due to drowsiness. The authors conclude confirming the therapeutic efficacy of Niaprazine in the treatment of behaviour disorders.