JDTic (dihydrochloride)

Modify Date: 2024-01-02 20:50:30

JDTic (dihydrochloride) Structure
JDTic (dihydrochloride) structure
Common Name JDTic (dihydrochloride)
CAS Number 785835-79-2 Molecular Weight 538.54900
Density N/A Boiling Point N/A
Molecular Formula C28H41Cl2N3O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of JDTic (dihydrochloride)


JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

 Names

Name (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
Synonym More Synonyms

 JDTic (dihydrochloride) Biological Activity

Description JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.
Related Catalog
In Vivo JDTic (2.5-16 mg/kg, s.c.) dose-dependently blocks the antinociceptive response of nicotine in the tail-flick test but has no effect in the hot-plate assay or body temperature assessments at any dose tested in the mice injected with nicotine[1]. JDTic (3 mg/kg, i.p.) is capable of reversing anxiety-like behavior in the rat model of hangover anxiety. JDTic (10 mg/kg, i.p.) decreases alcohol self-administration, suppresses cue-induced reinstatement of alcohol seeking, and specifically blocks the effects of a KOR agonist at the 2 h pretreatment time point[2]. JDTic (30 mg/kg, i.g.) significantly blockes U50,488-induced diuresis immediately in rats[3]. 
Animal Admin Mice: Naive mice are injected s.c. with JDTic (1, 4, 8, or 16 mg/kg) 18 h prior to nicotine (2.5 mg/kg, s.c.). Due to JDTic’s very long duration of action, an 18-h preinjection is chosen for the studies. Antinociception using the tail-flick and hot-plate tests is measured 5 min after nicotine injection or 20 min after morphine (8 mg/kg, s.c.), and changes in body temperature are measured 30 min after injection. To confirm an absence of mu antagonist effects by JDTic in these studies, JDTic (16 mg/kg) is also administered 1, 6, 18, and 24 h before morphine (8 mg/kg, s.c.) in the tail-flick test, and antinociception is measured 20 min after morphine.
References

[1]. Jackson KJ, et al. Effect of the selective kappa-opioid receptor antagonist JDTic on nicotine antinociception, reward, and withdrawal in the mouse. Psychopharmacology (Berl). 2010 Jun;210(2):285-94.

[2]. Schank JR, et al. The kappa opioid receptor antagonist JDTic attenuates alcohol seeking and withdrawal anxiety.Addict Biol. 2012 May;17(3):634-47. doi: 10.1111/j.1369-1600.2012.00455.x.

[3]. Beardsley PM, et al. Effectiveness of analogs of the 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) to reduce

 Chemical & Physical Properties

Molecular Formula C28H41Cl2N3O3
Molecular Weight 538.54900
Exact Mass 537.25200
PSA 88.32000
LogP 6.26360
Storage condition 2-8℃

 Synthetic Route

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JDTic (dihydrochloride) Structure

JDTic (dihydroc...

CAS#:785835-79-2

Literature: Thomas; Atkinson; Rothman; Fix; Mascarella; Vinson; Xu; Dersch; Lu; Cantrell; Zimmerman; Carroll Journal of Medicinal Chemistry, 2001 , vol. 44, # 17 p. 2687 - 2690

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JDTic (dihydrochloride) Structure

JDTic (dihydroc...

CAS#:785835-79-2

Literature: Thomas, James B.; Atkinson, Robert N.; Vinson, N. Ariane; Catanzaro, Jennifer L.; Perretta, Carin L.; Fix, Scott E.; Mascarella, S. Wayne; Rothman, Richard B.; Xu, Heng; Dersch, Christina M.; Cantrell, Buddy E.; Zimmerman, Dennis M.; Carroll, F. Ivy Journal of Medicinal Chemistry, 2003 , vol. 46, # 14 p. 3127 - 3137

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JDTic (dihydrochloride) Structure

JDTic (dihydroc...

CAS#:785835-79-2

Literature: Thomas, James B.; Atkinson, Robert N.; Vinson, N. Ariane; Catanzaro, Jennifer L.; Perretta, Carin L.; Fix, Scott E.; Mascarella, S. Wayne; Rothman, Richard B.; Xu, Heng; Dersch, Christina M.; Cantrell, Buddy E.; Zimmerman, Dennis M.; Carroll, F. Ivy Journal of Medicinal Chemistry, 2003 , vol. 46, # 14 p. 3127 - 3137

 Synonyms

(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 dihydrochloride
JDTic 2HCl|
1,2,3,4-tetrahydro-7-hydroxy-N-[(1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl]-(3R)-isoquinolinecarboxamide
JDTic (dihydrochloride)
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