Repositioning Candidate Details
| Candidate ID: | R1193 |
| Source ID: | DB09012 |
| Source Type: | experimental; withdrawn |
| Compound Type: | small molecule |
| Compound Name: | Carbazochrome |
| Synonyms: | 3-Hydroxy-1-methyl-5,6-inodlindionsemicarbazon; Adchnon; Adedolon; Adrenostan; Carbazochrome |
| Molecular Formula: | C10H12N4O3 |
| SMILES: | CN1CC(O)C2=C\C(=N\NC(N)=O)C(=O)C=C12 |
| Structure: |
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| DrugBank Description: | Carbazochrome is a hemostatic agent that promotes clotting, preventing blood loss from open wounds. It is an oxidation product of adrenaline which enhances the microcirculatory tone . In the future this may prevent excessive blood flow during surgical operations and the treatment of hemorrhoids, but research on effectiveness and severity of side effects remains inconclusive. It is not FDA-approved but is available as tablets or IM/SC injections in the treatment of hemorrhages in a number of countries. Carbazochrome has been investigated for use in the treatment of non-surgical acute uncomplicated hemorrhoids in a mixture with , and this combination therapy demonstrated efficacy and safe tolerability either at a local or systemic level . |
| CAS Number: | 69-81-8 |
| Molecular Weight: | 236.231 |
| DrugBank Indication: | Indicated for capillary and parenchymal hemorrhage (trauma, tonsillectomy, during surgery), intestinal bleeding, and thrombocytopenic purpura. |
| DrugBank Pharmacology: | Carbazochrome is an anti-bleeding agent that increases platelet aggregation and forms a platelet plug by interacting with α-adrenoreceptors on surface of platelets . It is shown to improve the structure of local capillary vessels in haemorrhage caused by fragility of capillaries. Carbazochrome capillary stabilizer that reverses pulmonary vascular hyperpermeability and decreases arterial PaO2 in experimental models . |
| DrugBank MoA: | Carbazochrome interacts with platelet surface α-adrenoreceptors which are Gq-coupled receptors that leads to activation of PLC IP3/DAG pathway and increase in intracellular calcium levels. Elevated calcium ions bind to calmodulin and activates Ca2+/calmodulin-dependent myosin light chain kinase, allowing the myosin crossbridge to bind to the actin filament and polymerisation of globular actin (G-actin) to filamentous actin (F-actin) . Subsequent contraction of endothelial cells changes the shape of platelets and promotes the release of factors such as serotonin, ADP, Von Willebrand and platelet activating factor by platelets that induce aggregation and platelet adherence . Carbazochrome is reported to inhibit vascular hyperpermeability by inhibiting agonist-induced phosphoinositides hydrolysis caused by various vasoactive agents such as tryptase, thrombin and bradykinin . |
| Targets: | -- |
| Inclusion Criteria: | Therapeutic strategy associated |
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