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(+)-SK&F 10047 hydrochloride

目录号 : GC17301

prototypical σ1 receptor agonist

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10mg
¥3,178.00
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50mg
¥13,328.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

IC50: N/A

SKF 10047 hydrochloride is a prototypical σ1 receptor agonist. Behaviorally active in animal models of memory and stress. It has been fully demonstrated that σ binding sites are distinct from phencyclidine binding sites on the NMDA receptor-ion channel complex, which has investigated extensively the functional role of σ receptors in the central nervous system [1,2].

In vitro: The effects of the stereoisomers of N-allylnormetazocine (SKF-10,047) were compared in rats on the hippocampal cholinergic functions. A putative σ1 receptor agonist, (+)-SKF-10,047, increased hippocampal extracellular acetylcholine level as well as anti-amnesic effect against scopolamine-induced memory dysfunctions in rats. Haloperidol, a putative σ1 receptor antagonist reversed these phenomena which were not produced by (-)-SKF-10,047. Such stereoselectivity and antagonism imply σ1 receptors involved in these (+)-SKF-10,047-stimulated hippocampal cholinergic functions [2].

In vivo: (+)-SKF-10,047 and dextromethorphan, being co-administered with phenytoin (10 mg/kg, an anticonvulsant drug), decreased conditioned fear stress with low doses (4 and 20 mg/kg, respectively). The effects were antagonized by the σ receptor antagonists, NE-100 and BMY-14802. Furthermore, the effects of (+)-SKF-10,047 or dextromethorphan plus phenytoin were inhibited by the dopamine D1 receptor antagonist (SCH 23390) and the dopamine D2 receptor antagonist ((-)-sulpiride), and they were also decreased by 6-hydroxydopamine-induced lesions of dopaminergic neurons. The ameliorating effects of (+)-SKF-10,047 and dextromethorphan on condition of fear stress using high doses (5 and 30 mg/kg, respectively) were also inhibited by both the dopamine receptor antagonists [3].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Walker JM, Bowen WD, Walker FO, Matsumoto RR, De Costa B, Rice KC.  Sigma receptors: biology and function. Pharmacol Rev. 1990 Dec;42(4):355-402.
[2] Matsuno K, Senda T, Kobayashi T, Mita S.  Involvement of sigma 1 receptor in (+)-N-allylnormetazocine-stimulated hippocampal cholinergic functions in rats. Brain Res. 1995 Sep 4; 690 (2): 200-6.
[3].  Kamei H, Kameyama T, Nabeshima T. (+)-SKF-10,047 and dextromethorphan ameliorate conditioned fear stress via dopaminergic systems linked to phenytoin-regulated sigma 1 sites. Eur J Pharmacol. 1996 Aug 8;309(2):149-58.

Chemical Properties

Cas No. 133005-41-1 SDF
化学名 3-allyl-6,11-dimethyl-1,2,3,4,5,6-hexahydro-2,6-methanobenzo[d]azocin-8-ol hydrochloride
Canonical SMILES OC1=CC2=C(C=C1)CC3N(CC=C)CCC2(C)C3C.Cl
分子式 C17H23NO.HCl 分子量 293.84
溶解度 <29.38mg/ml in Water; <29.38mg/ml in DMSO 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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