JDTic - CAS 361444-66-8
Catalog number:
361444-66-8
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H39N3O3
Molecular Weight:
465.64
COA:
Inquire
Targets:
Opioid Receptor
Description:
A 4-phenylpiperidine derivative, for the κ-opioid receptor.
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Purity:
≥98%
Appearance:
Solid powder
Synonyms:
(3R)-7-hydroxy-N-[1-[(3R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide;
Solubility:
Soluble in DMSO
Storage:
Store at 2-8 °C
MSDS:
Inquire
Application:
A selective opioid Kappa receptor antagonist.
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
ZLVXBBHTMQJRSX-LMUBNEGVSA-N
InChI:
1S/C28H39N3O3/c1-18(2)26(30-27(34)25-13-20-8-9-24(33)12-21(20)15-29-25)17-31-11-10-28(4,19(3)16-31)22-6-5-7-23(32)14-22/h5-9,12,14,18-19,25-26,29,32-33H,10-11,13,15-17H2,1-4H3,(H,30,34)/t19-,25+,26?,28?/m0/s1
Canonical SMILES:
CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(C(C)C)NC(=O)C3CC4=C(CN3)C=C(C=C4)O
Current Developer:
Eli Lilly
1.A Double-Blind, Placebo-Controlled Trial to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single, Escalating Oral Doses of JDTic.
Buda JJ1, Carroll FI2, Kosten TR3, Swearingen D4, Walters BB2. Neuropsychopharmacology. 2015 Aug;40(9):2059-65. doi: 10.1038/npp.2015.27. Epub 2015 Jan 23.
Animal studies suggest that kappa opioid receptor antagonists (KORAn) potentially could treat a wide variety of addictive and depressive disorders. We assessed the KORAn JDTic for safety, tolerability, and pharmacokinetics in a double-blind, placebo-controlled, randomized trial evaluating single oral doses in healthy adult males. Predose and postdose safety assessments included orthostatic vital signs; 6-lead continuous telemetry monitoring (approximately 16 h predose to 24 h postdose); 12-lead electrocardiograms (ECGs); clinical chemistry, hematology, coagulation, and urinalysis; psychomotor functioning (using the Wayne Saccadic Fixator (WSF)); and adverse events. As a potential indicator of JDTic effects on affect, the POMS Standard instrument was administered predose and daily postdose Days 1-6. At 1 mg, 2 of the 6 JDTic (and 0/6 placebo) subjects experienced a single, asymptomatic event of multiple beats of nonsustained ventricular tachycardia (NSVT).
2.Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents.
Carroll FI1, Gichinga MG2, Kormos CM2, Maitra R2, Runyon SP2, Thomas JB2, Mascarella SW2, Decker AM2, Navarro HA2. Bioorg Med Chem. 2015 Oct 1;23(19):6379-88. doi: 10.1016/j.bmc.2015.08.025. Epub 2015 Aug 25.
The design and discovery of JDTic as a potent and selective kappa opioid receptor antagonist used the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine pharmacophore as the lead structure. In order to determine if the 3-methyl or 4-methyl groups were necessary in JDTic and JDTic analogs for antagonistic activity, compounds 4a-c, and 4d-f which have either the 3-methyl or both the 3- and 4-methyl groups removed, respectively, from JDTic and analogs were synthesized and evaluated for their in vitro opioid receptor antagonist activities using a [(35)S]GTPγS binding assay. Other ADME properties were also assessed for selected compounds. These studies demonstrated that neither the 3-methyl or 3,4-dimethyl groups present in JDTic and analogs are required to produce potent and selective κ opioid receptor antagonists.
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CAS 361444-66-8 JDTic

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