2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. 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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Vedaclidine

Vedaclidine Chemical Structure

CAS No. : 141575-50-0

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Vedaclidine Related Antibodies

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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Description

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[1][2].

IC50 & Target[1]

mAChR1

 

mAChR2

 

mAChR3

 

mAChR4

 

mAChR5

 

In Vivo

Vedaclidine (0.3-10 mg/kg; p.o.; single administration) produces dose-dependent anti-hyperalgesic effects in the formalin-induced pain model[2].
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.

Animal Model: Sprague-Dawley (adult male, 200-250 g)[2]
Dosage: 0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg; 10 mg/kg
Administration: p.o.; single dose
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.
Animal Model: Sprague-Dawley (adult male, 250-300 g)[2]
Dosage: 0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg; 10 mg/kg
Administration: s.c.; single dose
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.
Animal Model: Sprague-Dawley (adult male, 80-100 g)[2]
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)
Administration: s.c.; single dose
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.
Animal Model: Sprague-Dawley (adult male, 200-250 g; 250-300 g)[2]
Dosage: 1.0 mg/kg; 3.0 mg/kg; 10 mg/kg
Administration: p.o.; single dose; s.c.; single dose
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.
Molecular Weight

283.46

Formula

C13H21N3S2
CAS No.
SMILES

CCCCSC1=NSN=C1[C@H]2C3CCN(CC3)C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Vedaclidine 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:

Vedaclidine141575-50-0mAChRMuscarinic acetylcholine receptormuscarinic M5 receptorsformalin-induced pain modelmuscarinic M2 receptorsneuropathic painmuscarinic M1 receptorsmuscarinic M3 receptorsinflammatory painmuscarinic M4 receptorscapsaicin-induced mechanical hyperalgesiaspinal cordInhibitorinhibitorinhibit

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