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Details

Stereochemistry ACHIRAL
Molecular Formula C28H24N6.2Br
Molecular Weight 604.338
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of FAZADINIUM BROMIDE

SMILES

[Br-].[Br-].CC1=C(N(\N=N\N2C3=[N+](C=CC=C3)C(C)=C2C4=CC=CC=C4)C5=[N+]1C=CC=C5)C6=CC=CC=C6

InChI

InChIKey=LBOZSXSPRGACHC-NFOZGECASA-L
InChI=1S/C28H24N6.2BrH/c1-21-27(23-13-5-3-6-14-23)33(25-17-9-11-19-31(21)25)29-30-34-26-18-10-12-20-32(26)22(2)28(34)24-15-7-4-8-16-24;;/h3-20H,1-2H3;2*1H/q+2;;/p-2/b30-29+;;

HIDE SMILES / InChI

Molecular Formula C28H24N6
Molecular Weight 444.5304
Charge 2
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Molecular Formula BrH
Molecular Weight 80.912
Charge 0
Count
MOL RATIO 2 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

Fazadinium (used as a bromide salt) is a muscle relaxant, which was applied in anesthesia under the name Fazadon. The current marketing status is unknown and the drug is supposed to be discontinued.

Originator

Approval Year

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
FAZADON

T1/2

ValueDoseCo-administeredAnalytePopulation
82 min
1 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens
153 min
1 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens
103 min
1 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens
30.2 min
0.5 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens
50.1 min
1 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens
76.4 min
1.5 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens
85 min
1 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens
140 min
1 mg/kg single, intravenous
FAZADINIUM plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
49%
FAZADINIUM serum
Homo sapiens
43%
FAZADINIUM serum
Homo sapiens

Doses

AEs

PubMed

Sample Use Guides

In Vivo Use Guide
The recommended dose is 1.5 mg/kg.
Route of Administration: Intravenous
In Vitro Use Guide
The guinea-pig isolated hypogastric nerve-vas deferens preparation and isolated phrenic nerve-diaphragm preparation were incubated with fazadinium at a concentration from 10(-5) to 3.2*10(-4) M. EC50 for neuromuscular blockade was 2.8*10(-5) M and EC50 for ganglion blockade was 6.4*10(-5) M.
Substance Class Chemical
Record UNII
8WV5538LFK
Record Status Validated (UNII)
Record Version