| Identification | Back Directory | [Name]
(-)-TRANS-(1S,2S)-U-50488 HYDROCHLORIDE POTENT K OPIOID RECEP | [CAS]
114528-79-9 | [Synonyms]
()-trans-(1S,2S)-U-50488
(-)-U-50488 hydrochloride
(?)-trans-(1S,2S)-U-50488 hydrochloride hydrate
(-)-trans-(1S,2S)-U-50488 hydrate hydrochloride
(-)-TRANS-(1S,2S)-U-50488 HYDROCHLORIDE POTENT K OPIOID RECEP
(-)-TRANS-(1S,2S)-U-50488 HYDROCHLORIDE POTENT K OPIOID RECEP
Benzeneacetamide,3,4-dichloro-N-methyl-N-[(1S,2S)-2-(1-pyrrolidinyl)cyclohexyl]-, hydrochloride(1:1)
trans-(1S,2S)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide hydrochloride hydrate
trans-(1S,2S)-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide hydrate hydrochloride | [Molecular Formula]
C19H26Cl2N2OHCl | [MDL Number]
MFCD00211360 | [MOL File]
114528-79-9.mol | [Molecular Weight]
405.79 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
H2O: soluble13mg/mL | [form ]
solid | [color ]
white | [optical activity]
[α]22/D 36.05°, c = 0.73 in methanol(lit.) | [Water Solubility ]
H2O: 13mg/mL |
| Hazard Information | Back Directory | [Uses]
(-)-U-50488 Hydrochloride is an analgesic agent used in the protection of ischemia/ischemia reperfusion. | [Uses]
(?)-trans-(1S,2S)-U-50488 hydrochloride hydrate (U-50488) has been used as a κ-opioid receptor (KOR) agonist has been used to study its effect on the increase of tidal volumes in adult red-eared slider turtles (Trachemys scripta). | [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]. | [Biochem/physiol Actions]
Potent κ opioid receptor agonist; more potent enantiomer of (±)-trans-U-50488. | [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. |
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