(+)-SK&F 10047 hydrochloride

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

Product information

CAS Number: 133005-41-1

Molecular Weight: 293.83

Formula: C17H24ClNO

Chemical Name: 1,13-dimethyl-10-(prop-2-en-1-yl)-10-azatricyclo[7.3.1.0²,⁷]trideca-2(7),3,5-trien-4-ol hydrochloride

Smiles: Cl.CC1C2CC3C=CC(O)=CC=3C1(C)CCN2CC=C

InChiKey: ZTGMHFIGNYXMJV-UHFFFAOYSA-N

InChi: InChI=1S/C17H23NO.ClH/c1-4-8-18-9-7-17(3)12(2)16(18)10-13-5-6-14(19)11-15(13)17;/h4-6,11-12,16,19H,1,7-10H2,2-3H3;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.