| Identification | Back Directory | [Name]
U-50488E | [CAS]
67197-96-0 | [Synonyms]
U-50488E
(+/-)-U-50488Hydrochloride
2-(3,4-dichlorophenyl)-N-methyl-N-[(1R,2R)-2-pyrrolidin-1-ylcyclohexyl]acetamide:hydrochloride | [Molecular Formula]
C19H27Cl3N2O | [MOL File]
67197-96-0.mol | [Molecular Weight]
405.79 |
| Chemical Properties | Back Directory | [storage temp. ]
Desiccate at -20°C | [solubility ]
<10.14mg/ml in H2O | [form ]
solid | [color ]
White | [Water Solubility ]
Soluble to 25 mM in water |
| Hazard Information | Back Directory | [Uses]
U-50488 Hydrochloride- D8 is a deuterated compound of (+/-)-U-50488 Hydrochloride (U850328). (+/-)-U-50488 Hydrochloride is a selective κ-opioid agonist and an analgesic agent (1,2). (+/-)-U-50488 Hydrochloride can be used to analyze structure-??activity relationships of kappa opioid receptors. | [Biological Activity]
(±)-u-50488 hydrochloride is a selective agonist for κ-opioid receptor [1].the κ-opioid receptor (kor) is a type of opioid receptor for opioid peptide dynorphin and controls addiction. also, kor plays an important role in stress, anxiety, anhedonia, depression and increased drug-seeking behavior.(±)-u-50488 hydrochloride is a selective kor agonist [1]. in isolated rat drg neurons, u-50488 (0.3-40 μm) inhibited voltage-independent ca2+ channel currents. in hela cells that didn’t express kor, u-50488 (20 μm) blocked ca2+ channels [2].in rhesus monkeys, u-50488 exhibited potent antinociceptive activity and produced diuresis [1]. u-50488 enhanced contraction of the rabbit vas deferens induced by electrically with ic50 value of 26.5 nm. in mice, u-50488 impaired motor function with ed50 value of 15.3 mg/kg and reduced spontaneous activity [3]. in adult rats, u-50488 increased the threshold required to maintain self-stimulation responding, a depressive-like effect. while, males were significantly more sensitive than females to the threshold-increasing effects [4]. | [storage]
Desiccate at -20°C | [References]
[1]. tang ah, collins rj. behavioral effects of a novel kappa opioid analgesic, u-50488, in rats and rhesus monkeys. psychopharmacology (berl), 1985, 85(3): 309-314.
[2]. hassan b, ruiz-velasco v. the κ-opioid receptor agonist u-50488 blocks ca2+ channels in a voltage- and g protein-independent manner in sensory neurons. reg anesth pain med, 2013, 38(1): 21-27.
[3]. lu sn, ma sc, zhang kg, et al. comparison of pharmacological profile of selective kappa-opioid agonist k-ii and u-50488. yao xue xue bao, 1991, 26(3): 171-174.
[4]. russell se, rachlin ab, smith kl, et al. sex differences in sensitivity to the depressive-like effects of the kappa opioid receptor agonist u-50488 in rats. biol psychiatry, 2014, 76(3): 213-222. |
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BOC Sciences
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https://www.bocsci.com |
| Company Name: |
Energy Chemical
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021-58432009 400-005-6266 |
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http://www.energy-chemical.com |
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