FSL0932
- Structure
- InChI=1S/C22H29NO5/c1-7-22(23(2)3,17-11-9-8-10-12-17)15-28-21(24)16-13-18(25-4)20(27-6)19(14-16)26-5/h8-14H,7,15H2,1-6H3
- InChIKey=LORDFXWUHHSAQU-UHFFFAOYSA-N
- Synonyms
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- Origin
- Chemically synthesized
- Biological activities
- Gastrointestinal peptides releasing (motilin)
Modulation of peptides (vasoactive intestinal peptide, gastrin , glucagon)
Opiate agonist (peripheral) μ, κ, δ
- Therapeutic
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Antimuscarinic
- Target
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Opiate receptors
- Assay information
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Inhibitory Effect on electrically evoked contraction (IC50 [μM]) : Guinea-pig ileum (4.7±0.2), Mouse vas deferens (21±2), Rabit vas deferens (>gt; 100 μM)
[3H]batrachotoxin binding displacement. (Ki = 2.66±0.15 μM)
Currents block in sensory neurons: Sodium currents (IC50 = 0.83±0.09 μM), Calcium currents (no effect), Potassium currents (23±6% block at 10 μM)
- References
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J. Pharmacol. Exp. Ther., 289: 1391-1397 (1999)
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J.Pharmacobio-Dyn., 13: 448-453 (1990)
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Francillon J, Philippe MP
[Trial in abdominal surgery of a new molecule, trimebutine, in resumption of postoperative transit].
Lyon Med, 225(4): 363-365 (1971) 5088602