Vedaclidine
Vedaclidine is an orally active muscarinic acetylcholine receptor (mAChR) modulator with mixed receptor activity, which activates muscarinic M2 and M4 receptors and blocks muscarinic M1, M3 and M5 receptors. Vedaclidine exerts its activity through interaction with spinal M4 muscarinic receptors, and does not induce hypothermia or excessive salivation. Vedaclidine can be used in research related to pain, neuropathic pain and inflammatory pain states.
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- No. CAS: 141575-50-0
- Fòrmula: C13H21N3S2
- Peso molecular:283.46
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
mAChR1 |
mAChR2 |
mAChR3 |
mAChR4 |
mAChR5 |
In Vivo
Vedaclidine (0.3-10 mg/kg; subcutaneous injection; single administration) dose-dependently reverses capsaicin-induced mechanical hyperalgesia[2].
Vedaclidine (0.1-30 mg/kg; subcutaneous injection; single administration) dose-dependently reverses carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia by activating muscarinic receptors, and exhibits synergistic analgesic effects when combined with Ketoprofen (HY-B0227)[2].
Vedaclidine (1.0-10 mg/kg; p.o.; s.c.; single administration) does not impair motor performance in the rotarod test at doses up to 10 mg/kg via oral or subcutaneous administration[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 (adult male, 200-250 g)[2]
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Dosage:0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Produced a dose-dependent reduction in formalin-induced paw licking.
Significantly reduced licking time in the early phase (0-5 minutes) at 10 mg/kg.
Significantly reduced licking time in the late phase (15-40 minutes) at 3.0 mg/kg and 10 mg/kg.
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Animal Model:Sprague-Dawley (adult male, 250-300 g)[2]
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Dosage:0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg; 10 mg/kg
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Administration:s.c.; single dose
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Result:Produced a dose-related reversal of capsaicin-induced mechanical hyperalgesia.
Significantly increased withdrawal thresholds at 3.0 mg/kg and 10 mg/kg.
Restored withdrawal thresholds to the maximum non-capsaicin injected level (~15 g) at 10 mg/kg.
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Animal Model:Sprague-Dawley (adult male, 80-100 g)[2]
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Dosage:0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg; 10 mg/kg; 30 mg/kg; 1.0 mg/kg (scopolamine combination)
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Administration:s.c.; single dose
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Result:Produced a dose-related reversal of carrageenan-induced thermal hyperalgesia, with significant effects at 0.3 mg/kg and higher.
Shifted the vedaclidine dose-response curve ~10-fold right for thermal hyperalgesia reversal when combined with 1.0 mg/kg s.c. scopolamine.
Produced a dose-related reversal of carrageenan-induced mechanical allodynia, with significant effects at 3.0-30 mg/kg.
Caused a modest right shift of the mechanical allodynia dose-response curve when combined with scopolamine.
Exhibited synergistic anti-thermal hyperalgesic effects with ketoprofen at fixed dose-ratios of 1:5, 1:10, and 1:30.
Had an ED50 of 0.45 mg/kg s.c. for thermal hyperalgesia reversal alone.
Demonstrated combination doses effective at levels inactive when administered alone.
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Animal Model:Sprague-Dawley (adult male, 200-250 g; 250-300 g)[2]
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Dosage:1.0 mg/kg; 3.0 mg/kg; 10 mg/kg
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Administration:p.o.; single dose; s.c.; single dose
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Result:Produced no significant effect on rotarod performance up to 2 hours post-administration at any tested dose via p.o. or s.c. routes.
Chemical Information
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No. CAS 141575-50-0
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Peso molecular 283.46
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Fòrmula C13H21N3S2
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SMILES
CCCCSC1=NSN=C1[C@H]2C3CCN(CC3)C2
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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.
Pureza y Documentación
Referencias
[1].
Eglen RM, et al. Muscarinic receptor ligands and their therapeutic potential. Curr Opin Chem Biol. 1999 Aug;3(4):426-32.
[Content Brief]
[2]. Shannon HE, et al. Antihyperalgesic effects of the muscarinic receptor ligand vedaclidine in models involving central sensitization in rats. Pain. 2001;93(3):221-227. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Vedaclidine Related Classifications
HY-183144 Related Classifications
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