mAChR
mAChRs (muscarinic acetylcholine receptors) are acetylcholine receptors that form G protein-receptor complexes in the cell membranes of certainneurons and other cells. They play several roles, including acting as the main end-receptor stimulated by acetylcholine released from postganglionic fibersin the parasympathetic nervous system. mAChRs are named as such because they are more sensitive to muscarine than to nicotine. Their counterparts are nicotinic acetylcholine receptors (nAChRs), receptor ion channels that are also important in the autonomic nervous system. Many drugs and other substances (for example pilocarpineand scopolamine) manipulate these two distinct receptors by acting as selective agonists or antagonists. Acetylcholine (ACh) is a neurotransmitter found extensively in the brain and the autonomic ganglia.
Targets for mAChR
Products for mAChR
- Cat.No. Product Name Information
- GC37731 Talsaclidine Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties.
- GC13618 Tarafenacin M3 muscarinic receptor antagonist
- GC16059 Tarafenacin D-tartrate Highly selective M3 muscarinic receptor antagonist
- GC37749 TBPB An allosteric agonist of M1 receptors
- GC31265 Tematropium (CDDD3602) Tematropium (CDDD3602) (CDDD3602) is a soft anticholinergics.
- GC31004 Temiverine hydrochloride Temiverine hydrochloride is a synthesized drug that is expected to have anticholinergic action.
- GC39186 Terodiline hydrochloride Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively.
- GC38950 Thiochrome Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer.
- GC32666 Timepidium bromide (Sesden) Timepidium bromide (Sesden) (Sesden; SA504) is an anticholinergic agent.
- GC13134 Tiotropium Bromide hydrate Muscarinic antagonist
- GC17954 Tolterodine tartrate Competitive muscarinic receptor antagonist
- GC12311 Trihexyphenidyl hydrochloride antiparkinsonian agent of the antimuscarinic class
- GC15150 Tropicamide Antimuscarinic drug
- GC17483 Trospium chloride Antimuscarinic agent
- GC31262 Vinconate (Chanodesethylapovincamine) Vinconate (Chanodesethylapovinc amine) is an indolonaphthyridine derivative and can stimulate the muscariic acetylcholine receptor.
- GC15990 VU 0238429 positive allosteric modulator of M5 receptors
- GC16655 VU 0357017 hydrochloride Positive allosteric modulator of muscarinic M1 receptors
- GC17821 VU 0365114 positive allosteric modulator of M5
- GC37928 VU 6008667 VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC50s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively.
- GC16819 VU0152100 M4 receptor allosteric modulators
- GC30809 VU0467154 A positive allosteric modulator of the M4 muscarinic acetylcholine receptor
- GC38957 VU0467485 VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM).
- GC64970 VU6000918 VU6000918 is a muscarinic acetylcholine (M4) positive allosteric modulator, with an EC50 of 19 nM for hM4.
- GC37932 VU6005806 VU6005806 (AZN-00016130) is a potent muscarnic acethylcholine receptor subtype 4 (M4) positive allosteric modulator (PAM), with EC50s of 94 nM, 28 nM, 87 nM and 68 nM for human, rat, dog and cyno M4, respectively.
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GC70135
VU6019650
VU6019650 is a potent and selective M5 mAChR positive allosteric modulator (IC50=36 nM) that can be used for research on alleviating opioid use disorder (OUD). VU6019650 has blood-brain barrier permeability and may regulate the mesolimbic dopamine reward circuit. VU6019650 can block the increase in firing rate of ventral tegmental area (VTA) dopamine neurons induced by Oxotremorine M iodide.
- GC67882 VU6028418
- GC18255 Xanomeline (oxalate) Muscarinic receptors are G protein-coupled acetylcholine receptors that play diverse roles.
- GC64243 Xanomeline tartrate Xanomeline (LY 246708) is the potent agonist of muscarinic M1/M4 receptor with antipsychotic-like activity.
- GC32416 YM-46303 YM-46303 is an mAChR antagonist which exhibits the highest affinities for M1 and M3 receptors, and selectivity for M3 over M2 receptor.
- GC30426 YM-58790 YM-58790 is a potent antagonist of M3 muscarinic receptor, with Ki of 15 nM.