AR-M 1000390 hydrochloride

AR-M 1000390 hydrochloride - Names and Identifiers

Name	N,N-Diethyl-4-(phenyl-4-piperidinylidenemethyl)benzamide Hydrochloride
Synonyms	ARM390 ARM-390 ARM 390 ARM-390HCl ARM390 HCl ARM390 Hydrochloride AR-M 1000390 hydrochloride N,N-Diethyl-4-(phenyl-4-piperidinylideneMethyl)benzaMide Hydrochloride N,N-Diethyl-4-(phenyl-4-piperidinylidenemethyl)benzamide Hydrochloride N,N-Diethyl-4-(phenyl(piperidin-4-ylidene)methyl)benzamide hydrochloride
CAS	209808-47-9

AR-M 1000390 hydrochloride - Physico-chemical Properties

Molecular Formula	C23H29ClN2O
Molar Mass	384.94216
Solubility	DMSO,H2O
Storage Condition	under inert gas (nitrogen or Argon) at 2-8°C
Use	AR-M 1000390 (hydrochloride), also known as ARM-390, is a low-internalizing nonpeptidic 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.
Target	EC50: 7.2±0.9 nM (δ opioid receptor)
In vitro study	AR-M 1000390 (Compound 6a) exhibits the binding affinities (IC 50 ) of 0.87±0.23 nM for the δ opioid receptor and extremely high selectivity over the µ receptor (IC 50 =3800±172 nM) and the κ receptor (IC 50 =7470±606 nM). RINm5F cells are treated with AR-M 1000390 (AR-M100390) and Cyclizine for 16-24 h before measurement of intracellular and secreted insulin levels. AR-M 1000390 mediates a dose-dependent decrease in insulin content with a maximal inhibition of ~90% at the highest concentration tested (10 μM).
In vivo study	Rats are treated with 5, 100, and 600 μmol/kg of AR-M 1000390 (AR-M100390) for 3 and/or 7 days; another group of rats treated with 600 μmol/kg of compound are allowed to recover for 14 days. AR-M 1000390 (600 μmol/kg) causes vacuolation in the β-cell of the rat pancreas that is associated with depletion of insulin and hyperglycemia after 7 days of dosing. Treatment of rats with 600 μmol/kg of AR-M 1000390 results in vacuolation of the β-cell of the rat pancreas that is similar to that reported for cyclizine and cyproheptadine.

AR-M 1000390 hydrochloride - Reference

Reference

1. Wei ZY, et al. N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues. J Med Chem. 2000 Oct 19;43(21):3895-905.2. Otieno MA, et al. Mechanistic investigation of N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)-benzamide-inducedinsulin depletion in the rat and RINm5F cells. Toxicol Sci. 2008 Sep;105(1):221-9.

AR-M 1000390 hydrochloride - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.598 ml	12.989 ml	25.978 ml
5 mM	0.52 ml	2.598 ml	5.196 ml
10 mM	0.26 ml	1.299 ml	2.598 ml
5 mM	0.052 ml	0.26 ml	0.52 ml

Last Update：2024-01-02 23:10:35

AR-M 1000390 hydrochloride - Reference Information

biological activity	AR-M 1000390 hydrochloride is an effective selective δ opioid receptor agonist with EC50 of 7.2±0.9 nM.
target	EC50: 7.2±0.9 nM (δ opioid receptor)

Last Update：2024-04-09 02:00:08