Naloxone benzoylhydrazone

Naloxone benzoylhydrazone用途

Naloxone benzoylhydrazone (NalBzoH) 是一种混合的激动剂/拮抗剂。Naloxone benzoylhydrazone 是原型 κ3 -阿片样受体激动剂,是克隆的 μ 和 δ 阿片样受体的部分激动剂,在阿片样 NOP 受体上是拮抗剂。Naloxone benzoylhydrazone 具有有效的镇痛作用。

Naloxone benzoylhydrazone名称

[ CAS 号 ]:
119630-94-3

[ 英文名 ]:
Naloxone benzoylhydrazone

[英文别名 ]:

naloxone benzoylhydrazone

Naloxone benzoylhydrazone生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

信号通路 >> 神经信号通路 >> 阿片受体

研究领域 >> 神经疾病

[ 靶点 ]

κ3-opioid receptor; μ- and δ-opioid receptors; Opioid-like NOP receptors[1][2]

[体外研究]

在μ阿片受体(MOR),纳洛酮苯甲酰腙刺激[35S] GTPγ-S结合(PEC50＝8.59)并抑制环AMP积累(PEC50＝8.74),其最大效应(EMAX)分别对应于与MOR激动剂DAMGO获得的55和65%(1)。在k-阿片受体(KOR)处,纳洛酮苯甲酰腙刺激[35S]GTPγS结合(pEC50=9.70)并抑制环腺苷酸形成(pEC50=9.45)[1]。在表达δ-阿片受体(DOR)的CHO细胞中,纳洛酮苯甲酰腙增加[35S]GTPγS结合(pEC50=8.49)并抑制环腺苷酸形成(pE50=8.61)[1]。

[体内研究]

在小鼠中,用固定剂量吗啡检查增加剂量的纳洛酮苯甲酰腙的镇痛研究显示了一个双相曲线。低至1μg/kg剂量的纳洛酮苯甲酰腙部分拮抗吗啡镇痛。较高剂量的纳洛酮苯甲酰腙继续以剂量依赖的方式抑制吗啡镇痛,1-mg/kg剂量完全拮抗吗啡镇痛。当纳洛酮苯甲酰腙剂量增加超过1毫克/千克时,镇痛恢复。纳洛酮苯甲酰腙在小鼠中单独给药时也产生类似的镇痛反应,在大鼠中也有活性。纳洛酮苯甲酰腙具有良好的p.o.活性,对小鼠的镇痛作用相当于s.c.给药。小剂量纳洛酮苯甲酰腙除阻断吗啡镇痛外,还部分逆转吗啡对小鼠胃肠道转运的抑制作用,完全拮抗吗啡对小鼠的致死作用,促进吗啡依赖小鼠的戒断[4]。

[参考文献]

[1]. Olianas MC, et al. Agonist activity of naloxone benzoylhydrazone at recombinant and native opioid receptors. Br J Pharmacol. 2006 Feb;147(4):360-70.

[2]. Connor M, et al. Has the sun set on kappa3-opioid receptors? Br J Pharmacol. 2006 Feb;147(4):349-50.

[3]. Paul D, et al. Naloxone benzoylhydrazone (NalBzoH) analgesia. J Pharmacol Exp Ther. 1990 Nov;255(2):769-74.

[4]. Gistrak MA, et al. Pharmacological actions of a novel mixed opiate agonist/antagonist: naloxone benzoylhydrazone. J Pharmacol Exp Ther. 1989 Nov;251(2):469-76.

Naloxone benzoylhydrazone物理化学性质

[ 密度 ]:
1.44g/cm3

[ 分子式 ]:
C₂₆H₂₇N₃O₄

[ 分子量 ]:
445.51000

[ 精确质量 ]:
445.20000

[ PSA ]:
94.39000

[ LogP ]:
2.84710

[ 折射率 ]:
1.722

Naloxone benzoylhydrazoneMSDS

详细MSDS(安全技术说明书)

Naloxone benzoylhydrazone安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

Naloxone benzoylhydrazone文献

The role of nociceptin in cognition.

Brain Res. 848(1-2) , 167-73, (1999)

The physiological role of the modulation via the nociceptin receptor is still unclear. Here we report the role of the nociceptin system in learning and memory. Nociceptin-knockout mice possess greater...

Agonist activity of naloxone benzoylhydrazone at recombinant and native opioid receptors.

Br. J. Pharmacol. 147(4) , 360-70, (2006)

1. In the present study, we examined the pharmacological activity of the putative kappa3-opioid receptor agonist naloxone benzoylhydrazone (NalBzoH) at recombinant human opioid receptors individually ...

Improvement by low doses of nociceptin on scopolamine-induced impairment of learning and/or memory.

Eur. J. Pharmacol. 395(2) , 149-56, (2000)

The effects of fmol doses of nociceptin/orphanin FQ on scopolamine-induced impairment of learning and/or memory were examined using spontaneous alternation of Y-maze and step-down type passive avoidan...

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