2. GPCR/G Protein Neuronal Signaling
  3. mAChR Cholinesterase (ChE)
  4. Trihexyphenidyl

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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Trihexyphenidyl

Trihexyphenidyl Chemical Structure

CAS No. : 144-11-6

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Trihexyphenidyl Related Antibodies

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Description

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.[1][2][3].

In Vitro

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 Related Antibodies
In Vivo

Trihexyphenidyl (i.v.) shows moderate selectivity for M1 muscarinic receptor-mediated ganglionic pressor responses over peripheral muscarinic receptor-mediated vagal bradycardia in pithed rats, with a selectivity ratio of 6[2].
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.

Animal Model: Sprague-Dawley (male, 200-300 g, pithed rat model)[2]
Dosage: Multiple intravenous doses (3-4 doses per experiment to generate ID50 and DR2 values)
Administration: i.v.
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.
Animal Model: Domestic cat (either sex, 3-4 kg, anaesthetized cat model)[2]
Dosage: Multiple intravenous doses (3-4 doses per experiment to generate ID50 values)
Administration: i.v.
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.
Molecular Weight

301.47

Formula

C20H31NO
CAS No.
SMILES

OC(C1=CC=CC=C1)(C2CCCCC2)CCN3CCCCC3
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Purity & Documentation
References
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Trihexyphenidyl Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trihexyphenidyl144-11-6mAChRCholinesterase (ChE)Muscarinic acetylcholine receptorrat peripheral glandular muscarinic receptorspithed ratsrat cerebral cortex M1 muscarinic receptorsrat peripheral cardiac muscarinic receptorsacetylcholinerat heart receptorsdystoniamuscarinic receptor antagonistParkinson's diseaserat submandibular gland receptorsInhibitorinhibitorinhibit

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