mAChR Activator

Guvacoline hydrochloride, a pyridine alkaloid found in Areca triandra, can act as a weak full agonist of atrial and ileal muscarinic receptors.

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.

Phytolaccagenin is a triterpenoid saponin aglycone, Antifungal agent, vasodilator, antihypertensive agent, and anti-inflammatory agent. Phytolaccagenin activates vascular and cardiac Muscarinic receptors, blocks cardiac β-adrenergic receptors, and inhibits voltage-dependent calcium channels in blood vessels. Phytolaccagenin inhibits the growth of Candida albicans and Cryptococcus neoformans. Phytolaccagenin induces vasodilation, produces negative inotropic and negative chronotropic effects, reduces mean arterial pressure, and inhibits LPS-induced inflammation. Phytolaccagenin exhibits enhanced antihypertensive effects in high salt-induced hypertensive rats. Phytolaccagenin can be used in the research of candidiasis, cryptococcosis, hypertension, and inflammation-related diseases.

LY 2033298 is a selective positive allosteric modulator of the muscarinic M₄ receptor. LY 2033298 can be used in the study of psychiatric disorders.

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.

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.

VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC₅₀ of 19 nM for hM4.

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.

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.

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.

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.

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.

(S)-Albuterol hydrochloride is a muscarinic receptor and phospholipase C activator. (S)-Albuterol hydrochloride increases intracellular free calcium in airway smooth muscle.

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 K_i 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

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.

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.

(S)-Albuterol is a muscarinic receptor and phospholipase C activator. (S)-Albuterol increases intracellular free calcium in airway smooth muscle.

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.

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.

Vinconate is an indolonaphthyridine derivative and can stimulate the muscariic acetylcholine receptor.