| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
mAChR1
M1 muscarinic acetylcholine receptor. Telenzepine is a potent, selective, and orally active M1 receptor antagonist. |
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| ln Vitro |
Telenzepine eliminates responses to either muscarine or the muscarinic component of the acetylcholine response at submicromolar doses (100 nM). Telenzepine (0.1-1000 nM) at doses inhibits the excitatory impact of muscarine at postsynaptic M1 receptors in a dose-dependent manner[2]. As an antagonist of muscarinic depolarization in AH/type 2 neurons, telenzepine has a threshold dosage between 0.1 and 1 nM. Telenzepine's IC50 of 8.5 nM is required to stop the reaction[2].
Telenzepine is a potent and selective M1 muscarinic receptor antagonist with a Ki of 0.94 nM. On a weight-for-weight basis, it is 25-50 times more potent than pirenzepine. Telenzepine binds to M1 receptors with high affinity and exhibits slow kinetics, which may contribute to its prolonged effect. The compound inhibits gastric acid secretion. |
| ln Vivo |
In the Ghosh-Schild rat (carbachol-stimulated), the chronic fistula rat (basal secretion), or the modified Shay rat (both intravenously and orally), intravenous telenzepine significantly suppresses gastric acid secretion[1]. The modified Shay rat exhibits much longer duration antiulcer effects when treated with telenzepine (2.7 μmol/kg; oral)[1].
In vivo, telenzepine inhibits gastric acid secretion and has anti-ulcer effects. It has been used in the treatment of peptic ulcers. The compound's effects are mediated through its selective antagonism of M1 muscarinic receptors. Telenzepine has been studied in patients with peptic ulcers and in various animal models of gastric acid hypersecretion. |
| Enzyme Assay |
In vitro receptor binding assays are performed to determine the affinity of telenzepine for the M1 receptor. Radioligand binding studies using membrane preparations from cells or tissues expressing the M1 receptor are conducted. The compound's ability to displace a specific radiolabeled ligand (e.g., [3H]-pirenzepine or [3H]-QNB) from the receptor is measured to calculate its Ki value. The selectivity of telenzepine for M1 over other mAChR subtypes is assessed by testing its activity at M2, M3, M4, and M5 receptors.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing recombinant M1 mAChR. The cells are treated with a receptor agonist in the presence or absence of varying concentrations of telenzepine. The inhibition of agonist-induced intracellular signaling, such as calcium mobilization or PI hydrolysis, is measured to quantify the antagonistic activity. The competitive nature of the antagonism is established by assessing the reversal of inhibition at high agonist concentrations. The compound's potency and affinity are determined from these functional and binding assays.
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| Animal Protocol |
In vivo studies are conducted in animal models and human subjects to evaluate the effects of telenzepine on gastric acid secretion. In pharmacokinetic studies, telenzepine is administered orally (e.g., 3 mg) to patients, and plasma levels are measured to determine Cmax, tmax, and AUC. Its effects on gastric acid secretion are evaluated by measuring acid output in response to various stimuli. The compound's anti-ulcer effects are assessed in models of gastric ulceration.
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| ADME/Pharmacokinetics |
Telenzepine is an orally active compound with a bioavailability of approximately 54%. Following a single oral dose of 3 mg telenzepine in patients with compensated liver cirrhosis, the mean maximal plasma level (Cmax) averaged 5.7 (1.9-10.1) ng/mL. After repeated dosing, some patients displayed different kinetic behavior resulting in higher AUC values on day 14/15 compared to day 1/2, while tmax and Cmax remained unchanged. The compound has a half-life for racemization of approximately 1000 years, indicating exceptional stereochemical stability.
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| Toxicity/Toxicokinetics |
Telenzepine is generally well-tolerated, but dose for dose it is more likely to have undesired anticholinergic effects compared to pirenzepine. Common side effects include dry mouth, blurred vision, and constipation, which are typical of muscarinic receptor antagonists. At higher doses, it may cause more pronounced anticholinergic effects. The compound's safety profile has been evaluated in clinical studies for the treatment of peptic ulcers.
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| References |
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| Additional Infomation |
1-Methyl-10-[2-(4-methyl-1-piperazinyl)-1-oxoethyl]-5H-thieno[3,4-b][1,5]benzodiazepine-4-one is a benzodiazepine drug.
Telenzepine is a potent, selective M1 muscarinic receptor antagonist that has been used in the treatment of peptic ulcers. It is a thienobenzodiazepine derivative that exhibits atropisomerism. Telenzepine is 25-50 times more potent than pirenzepine on a weight-for-weight basis. The compound is not approved for human therapeutic use in many countries and is primarily used as a research tool for studying M1 receptor function. |
| Molecular Formula |
C19H24CL2N4O2S
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|---|---|
| Molecular Weight |
443.39
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| Exact Mass |
442.1
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| CAS # |
147416-96-4
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| Related CAS # |
Telenzepine;80880-90-6
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| PubChem CID |
5387
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| Appearance |
White to off-white solid powder
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| Boiling Point |
544.7ºC at 760mmHg
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| Flash Point |
283.2ºC
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| Vapour Pressure |
6.34E-12mmHg at 25°C
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| LogP |
3.782
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
552
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VSWPGAIWKHPTKX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H22N4O2S/c1-13-18-14(12-26-13)19(25)20-15-5-3-4-6-16(15)23(18)17(24)11-22-9-7-21(2)8-10-22/h3-6,12H,7-11H2,1-2H3,(H,20,25)
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| Chemical Name |
1-methyl-10-[2-(4-methylpiperazin-1-yl)acetyl]-5H-thieno[3,4-b][1,5]benzodiazepin-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 62.5 mg/mL (140.96 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2554 mL | 11.2768 mL | 22.5535 mL | |
| 5 mM | 0.4511 mL | 2.2554 mL | 4.5107 mL | |
| 10 mM | 0.2255 mL | 1.1277 mL | 2.2554 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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