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AR-M 1000390 hydrochloride

Delta-opioid receptor agonist,low-internalizing CAS# 209808-47-9

AR-M 1000390 hydrochloride

Catalog No. BCC6143----Order now to get a substantial discount!

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Chemical structure

AR-M 1000390 hydrochloride

3D structure

Chemical Properties of AR-M 1000390 hydrochloride

Cas No. 209808-47-9 SDF Download SDF
PubChem ID 76848958 Appearance Powder
Formula C23H29ClN2O M.Wt 384.94
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 150 mg/mL (389.67 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name N,N-diethyl-4-[phenyl(piperidin-4-ylidene)methyl]benzamide;hydrochloride
SMILES CCN(CC)C(=O)C1=CC=C(C=C1)C(=C2CCNCC2)C3=CC=CC=C3.Cl
Standard InChIKey OTXTZCLQEGSAMW-UHFFFAOYSA-N
Standard InChI InChI=1S/C23H28N2O.ClH/c1-3-25(4-2)23(26)21-12-10-19(11-13-21)22(18-8-6-5-7-9-18)20-14-16-24-17-15-20;/h5-13,24H,3-4,14-17H2,1-2H3;1H
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 AR-M 1000390 hydrochloride

DescriptionNon-peptidic, low-internalizing δ-selective opioid receptor agonist; derivative of SNC 80. Does not trigger acute desensitization of the analgesic response; reduces CFA-induced hyperalgesia. Brain penetrant following systemic administration.

AR-M 1000390 hydrochloride Dilution Calculator

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AR-M 1000390 hydrochloride Molarity Calculator

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Preparing Stock Solutions of AR-M 1000390 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.5978 mL 12.989 mL 25.9781 mL 51.9561 mL 64.9452 mL
5 mM 0.5196 mL 2.5978 mL 5.1956 mL 10.3912 mL 12.989 mL
10 mM 0.2598 mL 1.2989 mL 2.5978 mL 5.1956 mL 6.4945 mL
50 mM 0.052 mL 0.2598 mL 0.5196 mL 1.0391 mL 1.2989 mL
100 mM 0.026 mL 0.1299 mL 0.2598 mL 0.5196 mL 0.6495 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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References on AR-M 1000390 hydrochloride

Ligand-directed trafficking of the delta-opioid receptor in vivo: two paths toward analgesic tolerance.[Pubmed:21147985]

J Neurosci. 2010 Dec 8;30(49):16459-68.

delta-Opioid receptors are G-protein-coupled receptors that regulate nociceptive and emotional responses. It has been well established that distinct agonists acting at the same G-protein-coupled receptor can engage different signaling or regulatory responses. This concept, known as biased agonism, has important biological and therapeutic implications. Ligand-biased responses are well described in cellular models, however, demonstrating the physiological relevance of biased agonism in vivo remains a major challenge. The aim of this study was to investigate the long-term consequences of ligand-biased trafficking of the delta-opioid receptor, at both the cellular and behavioral level. We used delta agonists with similar binding and analgesic properties, but high [SNC80 ((+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenz yl]-N,N-diethylbenzamide)]- or low [ARM390 (N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)-benzamide)]-internalization potencies. As we found previously, a single SNC80-but not ARM390-administration triggered acute desensitization of the analgesic response in mice. However, daily injections of either compound over 5 d produced full analgesic tolerance. SNC80-tolerant animals showed widespread receptor downregulation, and tolerance to analgesic, locomotor and anxiolytic effects of the agonist. Hence, internalization-dependent tolerance developed, as a result of generalized receptor degradation. In contrast, ARM390-tolerant mice showed intact receptor expression, but delta-opioid receptor coupling to Ca(2)+ channels was abolished in dorsal root ganglia. Concomitantly, tolerance developed for agonist-induced analgesia, but not locomotor or anxiolytic responses. Therefore, internalization-independent tolerance was produced by anatomically restricted adaptations leading to pain-specific tolerance. Hence, ligand-directed receptor trafficking of the delta-opioid receptor engages distinct adaptive responses, and this study reveals a novel aspect of biased agonism in vivo.

Pharmacological characterization of AR-M1000390 at human delta opioid receptors.[Pubmed:12875901]

Life Sci. 2003 Aug 15;73(13):1691-704.

We investigated the pharmacological properties of a newly synthesised delta agonist AR-M1000390, derived from SNC-80 ((+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethy l-benzamide), in the neuroblastoma cell line SK-N-BE expressing only human delta-opioid receptors. Binding and functional experiments showed a weak affinity (K(i) = 106 +/- 34 nM) correlated with a weak potency (EC(50) = 111 +/- 31 nM) to inhibit the forskolin-stimulated cAMP accumulation. Sustained activation of opioid receptors in the presence of the maximal inhibitory concentration of AR-M1000390 produced a rapid and strong desensitization. In order to examine the contribution of internalization and down-regulation in the desensitization processes, binding and functional experiments were conducted in the presence or in the absence of hypertonic sucrose solution to block clathrin-dependent opioid receptor endocytosis. We observed both the inability of AR-M1000390 to down-regulate opioid receptors and the absence of any effect of sucrose on desensitization. The lack of delta-opioid receptor internalization by AR-M1000390 was further corroborated by confocal microscopy using antibodies directed either against the endogenous delta-opioid receptors or the FLAG-tagged delta-opioid receptors stably expressed in the SK-N-BE cells. These data suggest that uncoupling rather than internalization is responsible for delta-opioid receptors desensitization by AR-M1000390.

Description

AR-M 1000390 hydrochloride is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.

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