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Pardoprunox hydrochloride(SLV-308 hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pardoprunox hydrochloride(SLV-308 hydrochloride)图片
CAS NO:269718-83-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Pardorunox (SLV-308) hydrochloride 是一种多巴胺 D2 和 D3 受体部分激动剂和血清素 5-HT1A 受体激动剂,pEC50 分别为 8、9.2 和 6.3。
Cas No.269718-83-4
别名盐酸帕多芦诺,SLV-308 hydrochloride; DU-126891 hydrochloride
Canonical SMILESO=C1OC2=C(N3CCN(C)CC3)C=CC=C2N1.[H]Cl
分子式C12H16ClN3O2
分子量269.73
溶解度DMF: 1 mg/ml,DMSO: 5 mg/ml,Ethanol: 0.1 mg/ml,PBS (pH 7.2): 5 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Pardoprunox hydrochloride is a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist, D2 (pKi = 8.1) and D3 receptor (pKi = 8.6) partial agonist and 5-HT1A receptor (pKi = 8.5) full agonist.IC50 value: 8.1/8.6/8.5 (pKi, for D2/ D3/5-HT1A receptor)Target: dopamine D2 and D3 receptor, 5-HT1A receptorin vitro: Pardoprunox also binds to D4 (pKi = 7.8), α1-adrenergic (pKi = 7.8), α2-adrenergic (pKi = 7.4), and 5-HT7 receptors (pKi = 7.2) with lower affinity. Pardoprunox acts as a potent but partial D(2) receptor agonist (pEC50 = 8.0 and pA2 = 8.4) with an efficacy of 50% on forskolin stimulated cAMP accumulation. At human recombinant dopamine D3 receptors, Pardoprunox acts as a partial agonist in the induction of [35S]GTPgammaS binding (intrinsic activity of 67%; pEC(50) = 9.2) and antagonized the dopamine induction of [35S]GTPgammaS binding (pA2 = 9.0). Pardoprunox acts as a full 5-HT1A receptor agonist on forskolin induced cAMP accumulation at cloned human 5-HT1A receptors but with low potency (pEC50 = 6.3) [1].in vivo: Pardoprunox induces contralateral turning behaviour in rats with unilateral 6-hydroxydopamine-induced lesions of the substantia nigra pars compacta (SNpc) (MED=0.03mg/kg; po). In MPTP-treated common marmosets, Pardoprunox dose-dependently increases locomotor activity (MED=0.03mg/kg; po) and decreases motor disability (MED=0.03mg/kg; po). In contrast Pardoprunox attenuated novelty-induced locomotor activity (MED=0.01mg/kg; po), (+)-amphetamine-induced hyperlocomotion (MED=0.3mg/kg; po) and apomorphine-induced climbing (MED=0.6mg/kg; po) in rodents. Pardoprunox also induces 5-HT1A receptor-mediated behaviours, including flat body posture and lower lip retraction (MED=0.3mg/kg; po). Collectively, these findings demonstrate that Pardoprunox possesses dopamine D2/3 partial agonist effects, 5-HT1A agonist effects and reduces parkinsonism in animal models. functional D2 receptor partial agonist activity and is effective in experimental models predictive of efficacy in PD.[2]

[1]. Glennon JC, et al. In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist. Synapse. 2006 Dec 15;60(8):599-608. [2]. Jones CA, et al. An in vivo pharmacological evaluation of pardoprunox (SLV308)--a novel combined dopamine D(2)/D(3) receptor partial agonist and 5-HT(1A) receptor agonist with efficacy in experimental models of Parkinson's disease. Eur Neuropsychopharmaco