114528-79-9 Usage
Description
(-)-TRANS-(1S,2S)-U-50488 HYDROCHLORIDE POTENT K OPIOID RECEP, also known as (-)-U-50488 Hydrochloride, is a potent κ-opioid receptor (KOR) agonist derived from the U-50,488 compound. It is characterized by its ability to selectively bind to and activate the κ-opioid receptors, which are involved in various physiological processes, including pain modulation and respiratory function.
Uses
Used in Pharmaceutical Industry:
(-)-TRANS-(1S,2S)-U-50488 HYDROCHLORIDE POTENT K OPIOID RECEP is used as an analgesic agent for the protection of ischemia/ischemia reperfusion. Its potent κ-opioid receptor agonist activity allows it to provide pain relief and protect tissues from damage during periods of reduced blood flow and subsequent reperfusion.
Used in Veterinary Medicine:
In the field of veterinary medicine, (-)-TRANS-(1S,2S)-U-50488 HYDROCHLORIDE POTENT K OPIOID RECEP has been utilized as a research tool to study its effects on the respiratory system. Specifically, it has been used to investigate the increase of tidal volumes in adult red-eared slider turtles (Trachemys scripta). This application helps researchers understand the role of κ-opioid receptors in respiratory function and may potentially lead to the development of new treatments for respiratory disorders in animals.
Please note that the provided materials do not mention any other industries where (-)-TRANS-(1S,2S)-U-50488 HYDROCHLORIDE POTENT K OPIOID RECEP is used. The information provided is limited to its applications in the pharmaceutical industry and veterinary medicine.
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.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 114528-79-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,1,4,5,2 and 8 respectively; the second part has 2 digits, 7 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 114528-79:
(8*1)+(7*1)+(6*4)+(5*5)+(4*2)+(3*8)+(2*7)+(1*9)=119
119 % 10 = 9
So 114528-79-9 is a valid CAS Registry Number.
114528-79-9Relevant articles and documents
Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488
Smith, Victoria C.,Cleghorn, Laura A. T.,Woodland, Andrew,Spinks, Daniel,Hallyburton, Irene,Collie, Iain T.,YiMok,Norval, Suzanne,Brenk, Ruth,Fairlamb, Alan H.,Frearson, Julie A.,Read, Kevin D.,Gilbert, Ian H.,Wyatt, Paul G.
, p. 1832 - 1840 (2012/06/18)
Screening of the Sigma-Aldrich Library of Pharmacologically Active Compounds (LOPAC) against cultured Trypanosoma brucei, the causative agent of African sleeping sickness, resulted in the identification of a number of compounds with selective antiproliferative activity over mammalian cells. These included (+)-(1R,2R)-U50488, a weak opioid agonist with an EC50 value of 59nM as determined in our T.brucei invitro assay reported previously. This paper describes the modification of key structural elements of U50488 to investigate structure-activity relationships (SAR) and to optimise the antiproliferative activity and pharmacokinetic properties of this compound.
