JDTic dihydrochloride

  • CAT Number: I004885
  • CAS Number: 785835-79-2
  • Molecular Formula: C28H41Cl2N3O3
  • Molecular Weight: 538.55
  • Purity: ≥95%
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<p style=/line-height:25px/>JDTic 2Hcl is a highly selective antagonist for the κ-opioid receptor; without affecting the μ- or δ-opioid receptors.<br>IC50 value:<br>Target: κ-opioid receptor<br>JDTic is a 4-phenylpiperidine derivative, distantly structurally related to analgesic drugs such as meperidine and ketobemidone, and more closely to the mu opioid antagonist alvimopan, and is structurally distinct from other kappa antagonists such as norbinaltorphimine. JDTic has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose, although its binding to the kappa opioid receptor is not irreversible and its long-acting effects are instead caused by altered activity of c-Jun N-terminal kinases. Animal studies suggest that it may produce antidepressant and anxiolytic effects, as well as having possible application in the treatment of addiction to cocaine and morphine.</p>

Catalog Number I004885
CAS Number 785835-79-2
Molecular Formula

C28H41Cl2N3O3

Purity 95%
Target Opioid Receptor
Solubility 10 mM in DMSO
Storage Store at -20°C
Reference

<p style=/line-height:25px/>
<br>[1]. Mitch, Charles H. et al. Discovery of Aminobenzyloxyarylamides as .kappa. Opioid Receptor Selective Antagonists: Application to Preclinical Development of a .kappa. Opioid Receptor Antagonist Receptor Occupancy Tracer. Journal of Medicinal Chemistry (2011), 54(23), 8000-8012.
<br>[2]. Schank JR, Goldstein AL, Rowe KE, King CE, Marusich JA, Wiley JL, Carroll FI, Thorsell A, Heilig M. 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.
<br>[3]. Wu H, Wacker D, Mileni M, Katritch V, Han GW, Vardy E, Liu W, Thompson AA, Huang XP, Carroll FI, Mascarella SW, Westkaemper RB, Mosier PD, Roth BL, Cherezov V, Stevens RC. Structure of the human κ-opioid receptor in complex with JDTic. Nature. 2012 Mar 21;485(7398):327-32. doi: 10.1038/nature10939.
<br>[4]. Beardsley PM, Pollard GT, Howard JL, Carroll FI. 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 U50,488-induced diuresis and stress-induced cocaine reinstatement in rats. Psychopharmacology (Berl). 2010 Jun;210(2):189-98.
<br>[5]. Jackson KJ, Carroll FI, Negus SS, Damaj MI. 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.
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