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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- No. CAS: 144-11-6
- Fòrmula: C20H31NO
- Peso molecular:301.47
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Publications Citing Use of MedChemExpress (MCE) Trihexyphenidyl
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Actividad biológica
Descripciòn
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. Further protocols information, click here.
In Vivo
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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No. CAS 144-11-6
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Peso molecular 301.47
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Fòrmula C20H31NO
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SMILES
OC(C1=CC=CC=C1)(C2CCCCC2)CCN3CCCCC3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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 -
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
Pureza y Documentación
Referencias
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Trihexyphenidyl Related Classifications
HY-B1277A Related Classifications
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Keywords
- 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