|Description||JDTic dihydrochloride is a highly selective antagonist for the κ-opioid receptor with IC50 value of 0.02nM without affecting the μ- or δ-opioid receptors. It is a 4-phenylpiperidine derivative and distantly structurally related to analgesic drugs such as meperidine and ketobemidone and more closely to the mu opioid antagonist alvimopan. It is structurally distinct from other kappa antagonists such as norbinaltorphimine. It is more selective and potent for KOR activity than other KOR antagonists. It is shown to block the antinociceptive response of nicotine in the tail-flick test with a dose-dependent manner. It can also block the nicotine withdrawal signs in mice via effecting the expression of a CPA associated with nicotine withdrawal. It is also reported to decrease the number of somatic withdrawal signs in morphine-dependent rats. It may produce antidepressant and anxiolytic effects and may be used in the treatment of addiction to cocaine and morphine.|
|Synonyms||JDTic (2HCl);(3R)-1,2,3,4-Tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-3-isoquinolinecarboxamide hydrochloride;(R)-7-hydroxy-N-((S)-1-((3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl)-3-methylbutan-2-yl)-1,2,3,4-tetrahydroisoquinoline-3-carboxamide;(3R)-7-hydroxy-N-[(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide;dihydrochloride|
|Solubility||10 mM in DMSO|
|Application||JDTic dihydrochloride is shown to block the antinociceptive response of nicotine in the tail-flick test with a dose-dependent manner. It can also block the nicotine withdrawal signs in mice via effecting the expression of a CPA associated with nicotine withdrawal. It is also reported to decrease the number of somatic withdrawal signs in morphine-dependent rats. It may produce antidepressant and anxiolytic effects and may be used in the treatment of addiction to cocaine and morphine.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
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