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Details

Stereochemistry RACEMIC
Molecular Formula C22H20FN3OS
Molecular Weight 393.477
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Tifluadom

SMILES

CN1C(CNC(=O)C2=CSC=C2)CN=C(C3=CC=CC=C3F)C4=CC=CC=C14

InChI

InChIKey=NPGABYHTDVGGJK-UHFFFAOYSA-N
InChI=1S/C22H20FN3OS/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)

HIDE SMILES / InChI

Molecular Formula C22H20FN3OS
Molecular Weight 393.477
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Description

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.

Originator

Approval Year

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
Dog: 5, 10, 20, 40, 80 micrograms/kg
Route of Administration: Oral
Substance Class Chemical
Record UNII
TF8X866L0I
Record Status Validated (UNII)
Record Version