JDTic
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| Surname | JDTic | |||||||||
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(3 R ) -7-Hydroxy- N - [(2 S ) -1 - [(3 R , 4 R ) -4- (3-hydroxyphenyl) -3,4-dimethylpiperidin-1-yl] -3-methylbutane -2-yl] -1,2,3,4-tetrahydroisoquinoline-3-carboxamide |
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| Molecular formula | C 28 H 39 N 3 O 3 | |||||||||
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| Molar mass | 465.626 g mol −1 | |||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||
JDTic is a selective and potent κ- opioid receptor - antagonist , which in science as an experimental drug and ligand is used. The effect of the antagonist, which is also active orally, which lasts for weeks, could be based on the activation of c-Jun-N-terminal kinases . Behavioral pharmacological studies suggest that JDTic has antidepressant, anxiolytic and addiction relieving effects.
Individual evidence
- ↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
- ↑ Thomas JB et al. (2001): Identification of the first trans- (3R, 4R) - dimethyl-4- (3-hydroxyphenyl) piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity, Journal of Medicinal Chemistry , 44 (17): 2687 -90. PMID 11495579
- ↑ Thomas JB et al. (2003): Identification of (3R) -7-hydroxy-N - ((1S) -1 - [[(3R, 4R) -4- (3-hydroxyphenyl) -3,4-dimethyl-1-piperidinyl] methyl ] -2-methylpropyl) -1,2,3,4-tetrahydro-3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist, Journal of Medicinal Chemistry , 46 (14): 3127-37. PMID 12825951
- ↑ Cai TB et al (2008): Synthesis and in vitro opioid receptor functional antagonism of analogues of the selective kappa opioid receptor antagonist (3R) -7-hydroxy-N - ((1S) -1 - {[(3R, 4R) -4- (3-hydroxyphenyl) -3,4-dimethyl-1-piperidinyl] methyl} -2-methylpropyl) -1,2,3,4-tetrahydro-3-isoquinolinecarboxamide (JDTic), Journal of Medicinal Chemistry , 51 (6): 1849-60. PMID 18307295
- ↑ Carroll FI et al. (2004): Pharmacological properties of JDTic: a novel kappa-opioid receptor antagonist, European Journal of Pharmacology , 501 (1-3): 111-9. PMID 15464069
- ↑ Bruchas MR (2007): Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase, Journal of Biological Chemistry , 282 (41): 29803-11. doi : 10.1074 / jbc.M705540200 PMID 17702750
- ↑ Knoll AT et al. (2007): Anxiolytic-like effects of kappa-opioid receptor antagonists in models of unlearned and learned fear in rats, Journal of Pharmacology and Experimental Therapeutics , 323 (3): 838-45. PMID 17823306
- ↑ Beardsley PM, Howard JL, Shelton KL, Carroll FI (2005): Differential effects of the novel kappa opioid receptor antagonist, JDTic, on reinstatement of cocaine-seeking induced by footshock stressors vs cocaine primes and its antidepressant-like effects in rats, Psychopharmacology (Berlin) , 183 (1): 118-26. doi : 10.1007 / s00213-005-0167-4 PMID 16184376
- ↑ Carroll FI, Harris LS, Aceto MD (2005): Effects of JDTic, a selective kappa-opioid receptor antagonist, on the development and expression of physical dependence on morphine using a rat continuous-infusion model, European Journal of Pharmacology , 524 ( 1-3): 89-94. PMID 16236279
- ↑ Jackson KJ, Carroll FI, Negus SS, Damaj MI (2010): Effect of the selective kappa-opioid receptor antagonist JDTic on nicotine antinociception, reward, and withdrawal in the mouse, Psychopharmacology (Berl) , 210 (2): 285- 94. PMID 20232057