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(+)-SK&F 10047 hydrochloride

prototypical σ1 receptor agonist CAS# 133005-41-1

(+)-SK&F 10047 hydrochloride

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Chemical structure

(+)-SK&F 10047 hydrochloride

3D structure

Chemical Properties of (+)-SK&F 10047 hydrochloride

Cas No. 133005-41-1 SDF Download SDF
PubChem ID 16759596 Appearance Powder
Formula C11H17N3O8 M.Wt 319.3
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in water and to 100 mM in DMSO
Chemical Name (1R,5R,6R,9S,11R,13S)-3-amino-14-(hydroxymethyl)-8,10-dioxa-2,4-diazatetracyclo[7.3.1.17,11.01,6]tetradec-3-ene-5,9,12,13,14-pentol
SMILES C(C1(C2C3C(N=C(NC34C(C1OC(C4O)(O2)O)O)N)O)O)O
Standard InChIKey CFMYXEVWODSLAX-CKYAAQHSSA-N
Standard InChI InChI=1S/C11H17N3O8/c12-8-13-6(17)2-4-9(19,1-15)5-3(16)10(2,14-8)7(18)11(20,21-4)22-5/h2-7,15-20H,1H2,(H3,12,13,14)/t2-,3?,4?,5-,6-,7+,9?,10-,11+/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of (+)-SK&F 10047 hydrochloride

DescriptionPrototypical σ1 receptor agonist. Behaviorally active in animal models of memory and stress.

(+)-SK&F 10047 hydrochloride Dilution Calculator

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Preparing Stock Solutions of (+)-SK&F 10047 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.1319 mL 15.6593 mL 31.3185 mL 62.637 mL 78.2963 mL
5 mM 0.6264 mL 3.1319 mL 6.2637 mL 12.5274 mL 15.6593 mL
10 mM 0.3132 mL 1.5659 mL 3.1319 mL 6.2637 mL 7.8296 mL
50 mM 0.0626 mL 0.3132 mL 0.6264 mL 1.2527 mL 1.5659 mL
100 mM 0.0313 mL 0.1566 mL 0.3132 mL 0.6264 mL 0.783 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on (+)-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 [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.

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References on (+)-SK&F 10047 hydrochloride

(+)-SKF-10,047 and dextromethorphan ameliorate conditioned fear stress via dopaminergic systems linked to phenytoin-regulated sigma 1 sites.[Pubmed:8874133]

Eur J Pharmacol. 1996 Aug 8;309(2):149-58.

Mice exhibited a marked suppression of motility when they were re-placed in the same environment in which they had previously received an electric footshock. (+)-SKF-10,047 ([2S-(2 alpha, 6 alpha, 11R*)]-1,2,3,4,5,6-hexahydro-6,11-dimethyl-3-(2-propenyl)-2,6-me tha no-3-benzazocin-8-ol hydrochloride; (+)-N-allylnormetazocine hydrochloride) and dextromethorphan, putative sigma receptor agonists, have been reported to reserve this psychological stress-induced motor suppression, defined as conditioned fear stress, through phenytoin-regulated type sigma 1, receptors. In the present study, we investigated the involvement of dopaminergic neurons in the ameliorating effects of (+)-SKF-10,047 and dextromethorphan on conditioned fear stress. (+)-SKF-10,047 and dextromethorphan attenuated conditioned fear stress at low doses (4 and 20 mg/kg, respectively) when they were co-administered with phenytoin (10 mg/kg), an anticonvulsant drug. The effects were antagonized by the sigma receptor antagonists. NE-100 (N,N-dipropyl-2-[4-methoxy-3-(2-phenylethoxy)phenyl]-ethylamine monohydrochloride) and BMY-14802 (a-(4-fluoro-phenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazine-butanol hydrochloride). Furthermore, the effects of (+)-SKF-10,047 or dextromethorphan in combination with phenytoin were blocked by the dopamine D1 receptor antagonist. SCH 23390 (R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3- benzazepine), and the dopamine D2 receptor antagonist, (-)-sulpiride, and they were also attenuated by 6-hydroxydopamine-induced lesions of dopaminergic neurons. The ameliorating effects of (+)-SKF-10,047 and dextromethorphan on conditioned fear stress at high doses (5 and 30 mg/kg, respectively) were also blocked by both the dopamine receptor antagonists. These results suggest that the stress-induced motor suppression is restored by the activation of dopaminergic neuronal systems as a result of the stimulation of phenytoin-regulated type sigma 1 receptors.

Involvement of sigma 1 receptor in (+)-N-allylnormetazocine-stimulated hippocampal cholinergic functions in rats.[Pubmed:8535837]

Brain Res. 1995 Sep 4;690(2):200-6.

The effects of the stereoisomers of N-allylnormetazocine (SKF-10,047) on the hippocampal cholinergic functions were compared in rats. A putative sigma 1 receptor agonist, (+)-SKF-10,047, elicited an increase of hippocampal extracellular acetylcholine level and anti-amnesic effect against scopolamine-induced memory dysfunctions in rats. These phenomena were not produced by (-)-SKF-10,047, and were reversed by haloperidol, a putative sigma 1 receptor antagonist. Such stereoselectivity and antagonism imply an involvement of sigma 1 receptors in these (+)-SKF-10,047-stimulated hippocampal cholinergic functions.

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