Talsaclidine
Based on 1 Customer Validation
Talsaclidine (WAL 2014 FU) is an orally active, blood-brain barrier-permeable muscarinic M1 receptor agonist. Talsaclidine activates the sympathetic nervous system and promotes adrenal catecholamine release in vivo. Talsaclidine exhibits extensive tissue distribution, kidney-dominant excretion and brain penetration properties, and it can be used in studies related to cholinergic signaling, cognitive function and Alzheimer's disease.
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- Reinheit : 98.75%
- CAS. Nr.: 147025-53-4
- Formel: C10H15NO
- Molecular Weight:165.24
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Speicherung:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
mAChR1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
2696 nM
Compound: Talsaclidine
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Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M3 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO | EC50 |
422 nM
Compound: Talsaclidine
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Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M5 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO | EC50 |
820 nM
Compound: Talsaclidine
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Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M1 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO | EC50 |
844 nM
Compound: Talsaclidine
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Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M4 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
| CHO | EC50 |
849 nM
Compound: Talsaclidine
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Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
Agonist activity at human muscarinic M2 receptor expressed in CHO cells after 30 mins by GTPgamma35S binding assay
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[PMID: 26299349] |
In Vitro
Talsaclidine (WAL 2014 FU) (0.1-12 μg/mL; 3 h) exhibits concentration-independent, very low plasma protein binding (<1%) in human plasma[1].
Talsaclidine acts as a partial agonist in isolated guinea pig tracheal muscle, with an intrinsic activity of 63% relative to carbachol and high susceptibility to functional antagonism by norepinephrine[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | AUC | MRT | T1/2 | CL | Vss | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1.2 mg/kg | i.v. | 442.5 ng/mL | 0.083 h | 154.2 ng·h/mL | 0.4 h | 1.0 h | 128 mL/min/kg | 3.2 L/kg | / |
| Rat[1] | 1.2 mg/kg | i.v. | 371.9 ng/mL | 0.083 h | 212.4 ng·h/mL | 1.0 h | 1.6 h | 92.2 | 5.7 L/kg | / |
| Rat[1] | 1.2 mg/kg | i.v. | 451.6 ng/mL | 0.083 h | 352.8 ng·h/mL | 1.2 h | 1.4 h | 55.5 mL/min/kg | 4 L/kg | / |
| Rhesus monkey[1] | 2.9 mg/kg | i.v. | 2645 ng/mL | 0.25 h | 5400 ng·h/mL | 3.9 h | 4.8 h | 10.6 mL/min/kg | 2.3 L/kg | / |
| Mice[1] | 5.9 mg/kg | p.o. | 1041 ng/mL | 0.25 h | 749.4 ng·h/mL | 1.3 h | 1.7 h | / | / | 99 % |
| Rat[1] | 5.9 mg/kg | p.o. | 846.8 ng/mL | 0.25 h | 963.7 ng·h/mL | 2.0 h | 3.2 h | / | / | / |
| Rat[1] | 5.9 mg/kg | p.o. | 1488 ng/mL | 0.25 h | 1623 ng·h/mL | 1.5 h | 4.4 h | / | / | / |
| Rat[1] | 5.9 mg/kg | p.o. | 9.5 ng/mL | 1.0 h | 27.7 ng·h/mL | 5.0 h | 4.7 h | / | / | / |
| Rhesus monkey[1] | 5.9 mg/kg | p.o. | 963.6 ng/mL | 2.8 h | 4152 ng·h/mL | 6.4 h | 3.7 h | / | / | / |
In Vivo
Talsaclidine (0.6, 1.2, 2.4 mg/kg; p.o.) is used in the delayed matching-to-sample (DMTS) test involving 7 aged rhesus monkeys. Among the doses, 0.6 mg/kg significantly increases DMTS accuracy at 8 h post-administration, and this improvement is independent of the time interval[3].
Talsaclidine (intravenous injection, 4-64 mg/kg) does not induce significant bronchospasm in intact anesthetized guinea pigs even at intravenous doses up to 64 mg/kg[4].
Talsaclidine induces bronchospasm in a dose-dependent manner, and its bronchospasmogenic activity shows no significant difference from that observed after β-adrenergic receptor blockade[4].
Talsaclidine (intravenous infusion at a dose of 1 mg/kg/min for up to 30 min) activates the sympathetic nervous system in anesthetized dogs, increases plasma adrenaline levels by more than 680-fold, elevates plasma norepinephrine and dopamine levels by 20-fold, and simultaneously induces hyperglycemia, increased renal vascular resistance, bradycardia, and accelerated respiratory rate[2].
Talsaclidine (1 mg/kg; intravenous injection) induces a biphasic blood pressure response and increases renal vascular resistance in anesthetized dogs. These effects are inhibited by α-adrenergic receptor blockade and muscarinic receptor blockade, and are also inhibited in a dose-dependent manner by the M1-selective antagonist Pirenzepine dihydrochloride (HY-17037)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Anaesthetized dogs[2]
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Dosage:1 mg/kg
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Administration:i.v.
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Result:Increased renal vascular resistance; the effect was inhibited by phentolamine and atropine.
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Animal Model:Seven aged rhesus macaques trained in a DMTS task[3]
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Dosage:0.6, 1.2, 2.4 mg/kg
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Administration:p.o.
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Result:0.6 mg/kg significantly improved DMTS accuracy 8 h after administration.
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Animal Model:Toliprolol- and atropine-pretreated guinea pigs[4]
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Dosage:4-64 mg/kg
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Administration:i.v.
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Result:Did not induce bronchospasm.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 147025-53-4
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Appearance Liquid (Density: 1.06±0.1 g/cm3)
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Molecular Weight 165.24
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Formel C10H15NO
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Color Light yellow to brown
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SMILES
C#CCO[C@@H]1[C@@H]2CCN(CC2)C1
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Synonyms
WAL 2014 FU free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 5 mg/mL (30.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
Verweise
[2]. Walland A, et al. In vivo consequences of M1-receptor activation by talsaclidine. Life sciences. 1997;60(13-14):977-84. [Content Brief]
[4]. Walland A, et al. Compensation of muscarinic bronchial effects of talsaclidine by concomitant sympathetic activation in guinea pigs. European journal of pharmacology. 1997 Jul 09;330(2-3):213-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 6.0518 mL | 30.2590 mL | 60.5180 mL | 151.2951 mL |
| 5 mM | 1.2104 mL | 6.0518 mL | 12.1036 mL | 30.2590 mL | |
| 10 mM | 0.6052 mL | 3.0259 mL | 6.0518 mL | 15.1295 mL | |
| 15 mM | 0.4035 mL | 2.0173 mL | 4.0345 mL | 10.0863 mL | |
| 20 mM | 0.3026 mL | 1.5130 mL | 3.0259 mL | 7.5648 mL | |
| 25 mM | 0.2421 mL | 1.2104 mL | 2.4207 mL | 6.0518 mL | |
| 30 mM | 0.2017 mL | 1.0086 mL | 2.0173 mL | 5.0432 mL |
Talsaclidine Related Classifications
HY-128855 Related Classifications
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