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Product Name:(+)-U-50488 hydrochloride
CAS:114528-81-3
Purity:≥99% by HPLC Remarks:(+)-U-50488 hydrochloride is the less active enantiomer of (±)-U-50488, which is an opioid receptor agonist.
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Product Name:(+)-U-50488 hydrochloride
CAS:114528-81-3
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Product Name:trans-(+)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide hydrochloride
CAS:114528-81-3
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| | (+)-U-50488 hydrochloride Basic information |
| | (+)-U-50488 hydrochloride Chemical Properties |
| storage temp. | Store at RT | | solubility | <40.58mg/ml in DMSO; <40.58mg/ml in H2O | | form | solid | | color | White |
| | (+)-U-50488 hydrochloride Usage And Synthesis |
| Uses | (+)-U-50488 Hydrochloride is a k-opioid agonist with no μ-opioid receptor effects in vitro, which may be used in the treatment of African trypanosomiasis. | | 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 | Store at RT | | 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. |
| | (+)-U-50488 hydrochloride Preparation Products And Raw materials |
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