Trihexyphenidyl
Based on 3 publication(s) in Google Scholar
Trihexyphenidyl is a selective and orally active M1 muscarinic receptor antagonist with an IC50 of 3.7 nM for rat cerebral cortex M1 muscarinic receptors. Trihexyphenidyl modulates cholinergic activity, countering acetylcholine supersensitivity in neural pathways. Trihexyphenidyl improves movement disorder, inhibits McN-A-343 (HY-107648)-induced pressor responses, vagally-induced bradycardia and vasodilatation. Trihexyphenidyl can be used for the research of Parkinson's disease..
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- CAS. Nr.: 144-11-6
- Formel: C20H31NO
- Molecular Weight:301.47
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Speicherung:
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Biologische Aktivität
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Trihexyphenidyl
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Biologische Aktivität
Trihexyphenidyl (Varying concentrations; 45 min) binds with highest affinity to rat cerebral cortex M1 muscarinic receptors (IC50 = 3.7 nM), moderate affinity to rat submandibular gland receptors (IC50 = 17 nM), and lowest affinity to rat heart receptors (IC50 = 31 nM), with a selectivity ratio of 8 for heart versus cortex receptors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Trihexyphenidyl (i.v.) shows moderate selectivity for M1 muscarinic receptor-mediated ganglionic nictitating membrane contractions over peripheral muscarinic receptor-mediated vagal bradycardia and vasodilatation in anaesthetized cats, with a selectivity ratio of 9[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 200-300 g, pithed rat model)[2]
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Dosage:Multiple intravenous doses (3-4 doses per experiment to generate ID50 and DR2 values)
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Administration:i.v.
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Result:Achieved an ID50 of 54 μg/kg for inhibiting McN-A-343 (HY-107648)-induced pressor responses.
Achieved an ID50 of 313 μg/kg for inhibiting vagally-induced bradycardia.
Exhibited a selectivity ratio (ID50 vagal bradycardia / ID50 McN-A-343 pressor response) of 6.
Achieved a DR2 value of 11.9 μg/kg for causing a 2-fold rightward shift of the McN-A-343 dose-response curve.
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Animal Model:Domestic cat (either sex, 3-4 kg, anaesthetized cat model)[2]
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Dosage:Multiple intravenous doses (3-4 doses per experiment to generate ID50 values)
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Administration:i.v.
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Result:Achieved an ID50 of 27 μg/kg for inhibiting McN-A-343-induced nictitating membrane contractions.
Achieved an ID50 of 257 μg/kg for inhibiting vagally-induced bradycardia.
Achieved an ID50 of 226 μg/kg for inhibiting vagally-induced vasodilatation.
Exhibited a selectivity ratio (ID50 vagal bradycardia / ID50 McN-A-343-induced ganglionic response) of 9.
Chemical Information
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CAS. Nr. 144-11-6
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Molecular Weight 301.47
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Formel C20H31NO
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SMILES
OC(C1=CC=CC=C1)(C2CCCCC2)CCN3CCCCC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
2020 Oct 20;117(42):26438-26447. PMID: 33024014 -
Sci Rep
Acetylcholine acts through M3 muscarinic receptor to activate the EGFR signaling and promotes gastric cancer cell proliferation. [Abstract]2017 Jan 19;7:40802. PMID: 28102288 -
Reinheit & Dokumentation
Verweise
[1]. Jabbari B, et al. Treatment of movement disorders with trihexyphenidyl[J]. Movement disorders: official journal of the Movement Disorder Society, 1989, 4(3): 202-212. [Content Brief]
[2]. Giachetti A, et al. Binding and functional profiles of the selective M1 muscarinic receptor antagonists trihexyphenidyl and dicyclomine. Br J Pharmacol. 1986;89(1):83-90. [Content Brief]
[3]. Takahashi S, et al. The effect of trihexyphenidyl, an anticholinergic agent, on regional cerebral blood flow and oxygen metabolism in patients with Parkinson's disease. J Neurol Sci. 1999;167(1):56-61. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Trihexyphenidyl Related Classifications
HY-B1277A Related Classifications
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- Trihexyphenidyl
- 144-11-6
- mAChR
- Cholinesterase (ChE)
- rat peripheral glandular muscarinic receptors
- pithed rats
- rat cerebral cortex M1 muscarinic receptors
- rat peripheral cardiac muscarinic receptors
- acetylcholine
- rat heart receptors
- dystonia
- muscarinic receptor antagonist
- Parkinson's disease
- rat submandibular gland receptors
- Inhibitor
- inhibitor
- inhibit