Details
| Stereochemistry | UNKNOWN |
| Molecular Formula | C20H31NO2.ClH |
| Molecular Weight | 353.927 |
| Optical Activity | ( + ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCN(CC)CCOC(=O)C(C1CCCCC1)C2=CC=CC=C2
InChI
InChIKey=WIELVDXKOYPANK-UHFFFAOYSA-N
InChI=1S/C20H31NO2.ClH/c1-3-21(4-2)15-16-23-20(22)19(17-11-7-5-8-12-17)18-13-9-6-10-14-18;/h5,7-8,11-12,18-19H,3-4,6,9-10,13-16H2,1-2H3;1H
Drofenine, product name Spasmo-Cibalgin (Novartis, Oman), is an antispasmodic/anticholinergic agent used for relaxing smooth muscle, treating dysmenorrhea, and relieving pain in the gastrointestinal tract, biliary passages, and urogenital tract. The possible therapeutic effect of drofenine is proposed by its activation of transient receptor potential vanilloid-3 (TRPV3), a member of the TRPV subfamily of TRP ion channels.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: Q8NET8 Gene ID: 162514.0 Gene Symbol: TRPV3 Target Organism: Homo sapiens (Human) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Spasmo Cibalgin Approved UseUnknown |
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| Primary | Spasmo Cibalgin Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Simultaneous determination of hydrochloride salts of adiphenine, diphenhydramine, ethyldiphenacetate, drofenine and promazine by ion-pair HPLC. | 1983 Aug |
|
| Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase. | 2001 Feb 1 |
|
| Drofenine: A 2-APB Analogue with Greater Selectivity for Human TRPV3. | 2014 Oct |
Sample Use Guides
Drofenine, was selective for TRPV3 in that activation of TRPA1, M8, V1, V2, and V4, which are known to be activated by the TRPV3 agonists 2-APB and/or carvacrol, was not observed at concentrations up to 1 mmol/L. A detectable change in TRPV3 activity was observed at concentrations as low as 30 μmol/L and increased in a concentration-dependent manner. At concentrations greater than 500 μmol/L, calcium flux exhibited some evidence of TRPV3 independence based on small and comparable responses in both native HEK-293 cells and other TRP channel overexpressing cell lines. The maximum change in cytosolic calcium (ΔF) for drofenine (EC50 = 207 μmol/L) was comparable to the known TRPV3 agonists 2-APB (EC50 = 78 μmol/L) and carvacrol (EC50 = 438 μmol/L).
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92806
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BT75TGU6AZ
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3146-19-8
Created by
admin on Sat Dec 16 09:24:31 GMT 2023 , Edited by admin on Sat Dec 16 09:24:31 GMT 2023
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SUBSTANCE RECORD
