2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. mAChR
  5. mAChR Activator

mAChR Activator

mAChR Isoform Comparison

mAChR Activators (19):

Cat. No. Product Name Effect Purity
  • HY-N5016
    Guvacoline hydrochloride
    		Activator 98.0%
    Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors.
  • HY-12158
    VU0238441
    		Activator 99.87%
    VU0238441 is a pan muscarinic acetylcholine receptor (mAChR) positive allosteric modulator (PAM) with EC50s of 3.2 μM, 2.8 μM, 2.2 μM, 2.1 μM, >10 μM for M1, M2, M3, M5 and M4, respectively.
  • HY-101841
    LY 2033298
    		Activator 99.87%
    LY 2033298 is a selective positive allosteric modulator of the muscarinic M4 receptor. LY 2033298 can be used in the study of psychiatric disorders.
  • HY-139044
    VU6000918
    		Activator 99.92%
    VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4.
  • HY-N4157
    Isopteropodine
    		Activator 99.13%
    Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research.
  • HY-N7247
    Thiochrome
    		Activator 99.89%
    Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
  • HY-176200
    VU6008055
    		Activator 99.43%
    VU6008055 (AF98943) is a brain-penetrant, orally active and selective muscarinic acetylcholine receptor subtype 4 (mAChR4) activator with human EC50 values of 73.4 nM. VU6008055 potentiates mAChR4 receptor activity in the presence of acetylcholine, and exhibits no activity at mAChR1, mAChR3, or mAChR5. VU6008055 can be used for the research of schizophrenia, parkinson’s disease, alzheimer’s disease.
  • HY-14563
    VU10010
    		Activator 98.04%
    VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus.
  • HY-N7421
    Smilagenin acetate
    		Activator 99.68%
    Smilagenin acetate is a sapogenin derivative extracted from patent US20030004147A1. Smilagenin acetate increases the expression of acetylcholine m2 receptors and can be used for the research of dementia.
  • HY-123778
    VU6007678
    		Activator
    VU6007678 is a CNS-penetrant muscarinic acetylcholine receptor (mAChR) modulator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke.
  • HY-183203
    VU0476406
    		Activator
    VU0476406 is a blood-brain barrier-permeable and selective muscarinic acetylcholine receptor subtype 4 (M4) activator with human EC50 of 91.0 nM and human pEC50 of 7.04. VU0476406 potentiates endogenous acetylcholine activity at M4 receptors. VU0476406 can be used for the research of Parkinson's disease.
  • HY-137311
    (S)-Albuterol hydrochloride
    		Activator
    (S)-Albuterol hydrochloride is a muscarinic receptor and phospholipase C activator. (S)-Albuterol hydrochloride increases intracellular free calcium in airway smooth muscle.
  • HY-175532
    M4 mAChR Modulator-2
    		Activator
    M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia
  • HY-N4157R
    Isopteropodine (Standard)
    		Activator
    Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M1 and 5-HT2 receptors. Isopteropodine has an EC50 of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research.
  • HY-181559S
    VU6025733
    		Activator
    VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M4 mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC50 of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease.
  • HY-137311A
    (S)-Albuterol
    		Activator
    (S)-Albuterol is a muscarinic receptor and phospholipase C activator. (S)-Albuterol increases intracellular free calcium in airway smooth muscle.
  • HY-101841R
    LY 2033298 (Standard)
    		Activator
    LY 2033298 (Standard) is the analytical standard of LY 2033298 (HY-101841). This product is intended for research and analytical applications. LY 2033298 is a selective positive allosteric modulator of the muscarinic M4 receptor. LY 2033298 can be used in the study of psychiatric disorders.
  • HY-N7247R
    Thiochrome (Standard)
    		Activator
    Thiochrome (Standard) is the analytical standard of Thiochrome. This product is intended for research and analytical applications. Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
  • HY-U00316
    Vinconate
    		Activator
    Vinconate is an indolonaphthyridine derivative and can stimulate the muscariic acetylcholine receptor.