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Hyoscyamine AChR inhibitor

Cat.No.S4014

Hyoscyamine (Daturine) is an AChR inhibitor with IC50 of 7.5 nM.
Hyoscyamine AChR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 289.37

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Quality Control

Batch: S401401 DMSO]58 mg/mL]false]Ethanol]58 mg/mL]false]Water]Insoluble]false Purity: 99.95%
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  • NMR
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99.95

Solubility

In vitro
Batch:

DMSO : 58 mg/mL (200.43 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 58 mg/mL

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 289.37 Formula

C17H23NO3

 Storage (From the date of receipt)
CAS No. 101-31-5 Download SDF Storage of Stock Solutions

Synonyms Daturine Smiles CN1C2CCC1CC(C2)OC(=O)C(CO)C3=CC=CC=C3

Mechanism of Action

Features
R-(+)-hyoscyamine is 30-fold lower in potency than that of the S-(-) enantiomer.
Targets/IC50/Ki
AChR
7.5 nM
In vitro
L-hyoscyamine increases the turnover number of GTPase activity from 0.19 min-1 to 2.11 min-1 in the steady-state kinetic measurements. R-(+)-hyoscyamine results in displacement of [3H]NMS binding to the muscarinic acetylcholine receptor subtypes (m1-m5) with pKi value of 8.67, 8.51, 7.46, 8.56 and 8.53, respectively. Hyoscyamine prevents the agonist-induced stimulation of cAMP production with EC50 of 7.8 nM in CHO cells. S-(-)-hyoscyamine enhances the forskolin-stimulated synthesis of cyclic AMP in rat cardiac (both atrial and ventricular) membranes by up to 24%.
In vivo
L-hyoscyamine (20 mg/kg) prolongs migrating myoelectric complex (MMC) cycle length from 17.6 min to 29.0 min in conscious rats.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/7797541/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12108922/
  • [6] https://pubmed.ncbi.nlm.nih.gov/12706477/

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