Secoverine
Secoverine is a muscarinic cholinergic receptor (mAChR) antagonist and antispasmodic with blood-brain barrier permeability. Secoverine binds competitively to muscarinic receptors, blocks central cholinergic effects, and inhibits cholinergically induced gastrointestinal motility, intestinal smooth muscle contraction, and acetylcholine-mediated neurotransmitter release. Secoverine exerts direct antispasmodic activity on intestinal smooth muscle independent of receptor blockade, and exhibits characteristics such as reversible smooth muscle activity and long duration of action. Secoverine can be used in studies related to hyperintestinal motility, diverticular disease, and colonic spasm.
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- CAS No.: 57558-44-8
- Formule: C22H35NO2
- Masse moléculaire:345.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Secoverine acts as a non-selective high-affinity muscarinic antagonist, exhibiting identical binding affinity for rat cardiac M2, rat cerebral cortex M1, and rat cerebral cortex M2 muscarinic receptors[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Secoverine (intravenous administration, dose 2.0-3.7 mg/kg) exhibits transient, slight mydriatic activity in female Swiss CPB mice[2].
Secoverine (intravenous injection, 3.48-6.81 mg/kg) potently antagonizes oxotremorine (HY-170032)-induced central tremor in male Swiss CPB mice, with ED50 values ranging from 3.48 to 6.81 mg/kg at 1 to 20 minutes post intravenous administration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar albino (male, 230-260 g, anaesthetized, bethanechol-induced intestinal hypermotility and secretion)[1]
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Dosage:10-8, 10-7, 10-6, 10-5, 10-4, 10-3 mol/kg (i.p.)
10-9, 10-8, 10-7, 10-6, 10-5 mol/kg (i.v.) -
Administration:i.p. (simultaneously with bethanechol; 25 minutes before bethanechol)
i.v. (simultaneously with bethanechol) -
Result:Failed to block bethanechol-triggered fluid secretion at 10-3 mol/kg via intraperitoneal co-injection.
Suppressed bethanechol-triggered fluid secretion at 10-5 mol/kg and 10-4 mol/kg with intraperitoneal pre-injection 25 min earlier.
Suppressed bethanechol-triggered hyperpolarization at 10-4 mol/kg with intraperitoneal pre-injection 25 min earlier.
Suppressed bethanechol-triggered hypermotility at 10-7 mol/kg, and fully blocked the response at 10-4 mol/kg with intraperitoneal pre-injection 25 min earlier.
Blocked bethanechol-triggered hyperpolarization at 10-5 mol/kg via intravenous co-injection.
Blocked bethanechol-triggered hypermotility at 10-7 mol/kg via intravenous co-injection.
Chemical Information
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CAS No. 57558-44-8
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Masse moléculaire 345.52
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Formule C22H35NO2
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SMILES
O=C(C1CCCCC1)CCCN(C(CC2=CC=C(C=C2)OC)C)CC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Greenwood B, et al. Effect of secoverine and atropine on intestinal secretion and motor activity in the rat small intestine in-vivo. The Journal of pharmacy and pharmacology. 1984 Feb;36(2):100-6. [Content Brief]
[2]. Zwagemakers JM, et al. Secoverine selectively antagonizes muscarinic effects in various in vivo preparations. European journal of pharmacology. 1981 Apr 24;71(1):165-8. [Content Brief]
[3]. Brunner F, et al. Secoverine is a non-selective muscarinic antagonist on rat heart and brain receptors. European journal of pharmacology. 1986 Aug 07;127(1-2):17-25. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Secoverine Related Classifications
HY-183540 Related Classifications
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