尼普拉嗪 T36949

Product Introduction
Bioactivity


英文名: Niaprazine

描述: Niaprazine 是有效的组胺 H1 受体拮抗剂，具有抗组胺和抗血清素活性。Niaprazine 在睡眠障碍方面有研究的价值。

体外活性: Niaprazine，特别是（+）立体异构体，在alpha 1（Ki = 77 nM）和5-HT2（Ki = 25 nM）结合位点上具有较高的亲和力，但在5-HT1A和5-HT1B结合位点上的识别能力较差（Ki > 微米级）[1]。

体内活性: 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[2].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (280.55 mM)


关键字: 5-HIAA | disorders | sleep | autistic | Histamine Receptor | inhibit | 5-HT2 | sedative | Inhibitor | H1-receptor | Niaprazine

相关产品: Naftopidil dihydrochloride | Sulamserod | Tiflucarbine | Pirenperone | Zacopride hydrochloride | idalopirdine | Sumatriptan succinate | H-9 dihydrochloride | (+)-OSU 6162 | 2-Bromo-6-methoxynaphthalene

相关库: Neurotransmitter Receptor Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | GPCR Compound Library | Serotonin Receptor-Targeted Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途