Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C22H20FN3OS.ClH |
| Molecular Weight | 429.938 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1C(CNC(=O)C2=CSC=C2)CN=C(C3=CC=CC=C3F)C4=CC=CC=C14
InChI
InChIKey=JFZSUQQSHDYRGA-UHFFFAOYSA-N
InChI=1S/C22H20FN3OS.ClH/c1-26-16(13-25-22(27)15-10-11-28-14-15)12-24-21(17-6-2-4-8-19(17)23)18-7-3-5-9-20(18)26;/h2-11,14,16H,12-13H2,1H3,(H,25,27);1H
Tifluadom is an opioid benzodiazepine with potent analgesic activity. Studies using antagonists for κ-, δ-, and μ-opiate receptors in guinea pig myenteric plexus-longitudinal muscle preparation and mouse and rabbit vasa deferentia showed that Tifluadom is an opioid analgesic with a preference for opiate κ-receptors. In rat brain homogenates, tifluadom displaced kappa-antagonist naloxone from its binding sites with an IC50 of 12nM but had no effect on flunitrazepam binding. Tifluadom produced a dose-related diuresis in normally hydrated rats and the diuretic effect was antagonized by naloxone and blocked by morphine administration.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| An opioid benzodiazepine. | 1982 Aug 19 |
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| Unexpected opioid activity in a known class of drug. | 1982 Sep 20-27 |
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| Studies on the adrenomedullary dependence of kappa-opioid agonist-induced diuresis in conscious rats. | 1989 Dec |
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| Differential effects of fedotozine compared to other kappa agonists on diuresis in rats. | 1996 Dec |
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| Activation of the cloned human kappa opioid receptor by agonists enhances [35S]GTPgammaS binding to membranes: determination of potencies and efficacies of ligands. | 1997 Aug |
|
| Enantiomers of 2-[(Acylamino)ethyl]-1,4-benzodiazepines, potent ligands of kappa-opioid receptor: chiral chromatographic resolution, configurational assignment and biological activity. | 2001 |
|
| Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity. | 2003 Aug 28 |
Patents
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RQB9JWT8M3
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71752575
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96337-50-7
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DTXSID80858485
Created by
admin on Sat Dec 16 10:15:03 GMT 2023 , Edited by admin on Sat Dec 16 10:15:03 GMT 2023
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SUBSTANCE RECORD
