361444-66-8
Chemical Structure
JDTic
- CAS No.: 361444-66-8
- Formula:C28H39N3O3
- Molecular Weight:465.63
IUPAC Name: (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
InChIKey: ZLVXBBHTMQJRSX-VMGNSXQWSA-N
SMILES: O=C([C@@H]1NCC2=C(C=CC(O)=C2)C1)N[C@@H](C(C)C)CN3C[C@H](C)[C@](C)(C4=CC=CC(O)=C4)CC3
Biological Activity: JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal[1][2][3].
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JDTic | JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal. | |||||||||||||||||||||
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- [1]. Carroll FI, et al. Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents. Bioorg Med Chem. 2015;23(19):6379-6388. [Content Brief]
- [2]. Chavkin C, et al. Kappa antagonist JDTic in phase 1 clinical trial[J]. Neuropsychopharmacology, 2015, 40(9): 2057-2058.
- [3]. Wu H, et al. Structure of the human κ-opioid receptor in complex with JDTic[J]. Nature, 2012, 485(7398): 327-332.
Keywords
