Melperone (hydrochloride) (Synonyms:盐酸美哌隆)
目录号 : KCM11811 CAS No. : 1622-79-3 纯度 : ≥98%
Melperone is an atypical antipsychotic. It binds to α- and α-adrenergic and dopamine D receptors (Ks = 180, 150, and 180 nM, respectively), as well as the serotonin (5-HT) receptor subtype 5-HT (K = 102 nM). It is selective for these receptors over histamine H, muscarinic, 5-HT, 5-HT, and 5-HT receptors (Ks = 580, >10,000, 2,200, 3,400, and 2,100 nM, respectively). Melperone (2 mg/kg per day) increases basal, but not amphetamine-induced, extracellular dopamine levels in the rat nucleus accumbens.
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100mg
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250mg
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1g
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5g 询价 In-stock

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生物活性

Melperone (hydrochloride) is a butyrophenone with atypical antipsychotic properties. Melperone (hydrochloride) is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone (hydrochloride) has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone (hydrochloride) can be used for the study of schizophrenia, and agitation in the elderly[1].

IC50&Target

5-HT1A Receptor                      5-HT1D Receptor                 5-HT2A Receptor               5-HT2C Receptor

Human D2 Receptor                α1-adrenergic receptor         α2-adrenergic receptor       CYP2D6

180 nM (Kd)                             180 nM (Kd)                          150 nM (Kd)

体内研究

Melperone (2 mg/kg/day; drinking water; Replace the water bottle twice a week in a dark place; Hydrochloride can increase the basal extracellular dopamine levels in the rat nucleus accumbens for 21 days, but does not affect the extracellular dopamine levels induced by D-amphetamine [1].

 

Animal Model: Male Sprague-Dawley albino rats (180-200 g) was administered subcutaneously with D-Amphetamine sulfate (1.0 mg/kg)[1]
Dosage: 2 mg/kg/day
Administration: Drinking water; changed in lightproof drinking bottles twice a week; for 21 days
Result: Increased basal extracellular DA and enhanced D-Amphetamine-induced DA release in the striatum.
 
分子式
C16H22FNO.HCl
分子量
299.81
CAS号
1622-79-3
中文名称
盐酸美哌隆
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (166.77 mM; Need ultrasonic and warming)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 3.3354 mL 16.6772 mL 33.3545 mL
5 mM 0.6671 mL 3.3354 mL 6.6709 mL
10 mM 0.3335 mL 1.6677 mL 3.3354 mL
*

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, 6 months; -20°C, 1 month。-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。

[1]. Lurasidone Improves Psychopathology and Cognition in Treatment-Resistant Schizophrenia 

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