891-60-1
Chemical Structure
Declopramide
Synonym(s): 3-Chloroprocainamide
- CAS No.: 891-60-1
- Formula:C13H20ClN3O
- Molecular Weight:269.77
IUPAC Name: 4-amino-3-chloro-N-(2-(diethylamino)ethyl)benzamide
InChIKey: YEYAKZXEBSVURO-UHFFFAOYSA-N
SMILES: O=C(NCCN(CC)CC)C1=CC=C(N)C(Cl)=C1
Biological Activity: Declopramide (3-Chloroprocainamide) is an orally active, blood-brain barrier-permeable IκBβ/NF-κB inhibitor and chemosensitizer. Declopramide exhibits affinity for rabbit 5-HT3 receptors (5-HT3R) with a Ki value of 3.2 μM. Declopramide inhibits IκBβ degradation, blocks NFκB activation, and induces rapid apoptosis and DNA strand breaks in cancer cells. Declopramide enhances the cytotoxicity induced by Cisplatin (HY-17394) and is also metabolically converted to N-acetyl declopramide. Declopramide can be used in the research of tumors such as brain astrocytoma[1][2][3].
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Declopramide | Declopramide (3-Chloroprocainamide) is an orally active, blood-brain barrier-permeable IκBβ/NF-κB inhibitor and chemosensitizer. Declopramide exhibits affinity for rabbit 5-HT3 receptors (5-HT3R) with a Ki value of 3.2 μM. Declopramide inhibits IκBβ degradation, blocks NFκB activation, and induces rapid apoptosis and DNA strand breaks in cancer cells. Declopramide enhances the cytotoxicity induced by Cisplatin (HY-17394) and is also metabolically converted to N-acetyl declopramide. Declopramide can be used in the research of tumors such as brain astrocytoma. | |||||||||||||||||||||
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References
- [1]. Liberg D, et al. N-substituted benzamides inhibit NFkappaB activation and induce apoptosis by separate mechanisms. British journal of cancer. 1999 Nov;81(6):981-8. [Content Brief]
- [2]. Hua J, et al. Comparison of antitumor activity of declopramide (3-chloroprocainamide) and N-acetyl-declopramide. Anticancer research. 1999;19(1A):285-90. [Content Brief]
- [3]. Hua J, et al. Pharmacokinetics and central nervous system toxicity of declopramide (3-chloroprocainamide) in rats and mice. Anti-cancer drugs. 1999 Jan;10(1):79-88. [Content Brief]
