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Details

Stereochemistry RACEMIC
Molecular Formula C10H11N4O5S.Na
Molecular Weight 322.273
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of CARBAZOCHROME SODIUM SULFONATE

SMILES

[Na+].CN1C(CC2=C\C(=N\NC(N)=O)C(=O)C=C12)S([O-])(=O)=O

InChI

InChIKey=HLFCZZKCHVSOAP-DAMYXMBDSA-M
InChI=1S/C10H12N4O5S.Na/c1-14-7-4-8(15)6(12-13-10(11)16)2-5(7)3-9(14)20(17,18)19;/h2,4,9H,3H2,1H3,(H3,11,13,16)(H,17,18,19);/q;+1/p-1/b12-6-;

HIDE SMILES / InChI

Molecular Formula Na
Molecular Weight 22.98976928
Charge 1
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula C10H11N4O5S
Molecular Weight 299.283
Charge -1
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 1
Optical Activity ( + / - )

Description

Carbazochrome Sulfonic Acid is an antihemorrhagic, or hemostatic, agent that will cease blood flow by causing the aggregation and adhesion of platelets in the blood to form a platelet plug, ceasing blood flow from an open wound. It is hoped that this drug can be used in the future for preventing excessive blood flow during surgical operations and the treatment of hemorrhoids, but research on its effectiveness and the severity of possible side effects remains to be fairly inconclusive. Carbazochrome has been investigated for use in the treatment of hemorrhoids in a mixture with troxerutin. Carbazochrome interacts with α-adrenoreceptors on surface of platelets, which are coupled to Gq protein and initiate PLC IP3/DAG pathway to increase intracellular free calcium concentration with these subsequent actions: Activates PLA2 and induce arachidonic acid pathway to synthese endoperoxides (TxA2, thromboxane A2); Calcium binds to calmodulin which then binds and activates myosin light-chain kinase, that will enable the myosin crossbridge to bind to the actin filament and allow contraction to begin. This will change platelet’s shape and induce release of serotonin, ADP, vWF (Von Willebrand factor), PAF (Platelet-activating factor) to promote further aggregation and adhesion. Carbazochrome is usually used to treat bleeding tendency (for example purpura, etc.) caused by attenuation of microvascular resistance, bleeding from skin or mucosa and inner membrane, fundal/renal/uterine bleeding and intraoperative or postoperative abnormal bleeding.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Unknown
Preventing
ADONA
Preventing
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
19.4 ng/mL
90 mg single, oral
CARBAZOCHROME plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
77.94 ng × h/mL
90 mg single, oral
CARBAZOCHROME plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
1.64 h
90 mg single, oral
CARBAZOCHROME plasma
Homo sapiens

PubMed

Sample Use Guides

In Vivo Use Guide
Unknown
Route of Administration: Unknown
In Vitro Use Guide
Unknown
Substance Class Chemical
Record UNII
J0I08M946E
Record Status Validated (UNII)
Record Version