- Cat. No.
- A13761
(-)-Nicotine ditartrate
(-)-Nicotine ditartrate is a potent agonist of AChR (nicotinic acetylcholine recepto).
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Muscarinic acetylcholine receptors (mAChRs) are a class of G protein-coupled receptors (GPCRs) found in the central and peripheral nervous systems, as well as in various other tissues and organs throughout the body. These receptors are named after muscarine, a natural alkaloid compound found in certain mushrooms, which was one of the first substances discovered to activate them.
There are five subtypes of muscarinic receptors, designated as M1 through M5, each with distinct tissue distribution and functions. Here's an overview of their roles:
Muscarinic receptors are activated by the neurotransmitter acetylcholine and play a vital role in regulating a wide range of physiological processes, including heart rate, smooth muscle contraction, glandular secretion, and neurotransmitter release. They are targets for various drugs, including anticholinergic agents, which block their activity, and drugs used to treat conditions like bradycardia and neurodegenerative disorders.
Understanding the functions and regulation of muscarinic acetylcholine receptors is essential for developing therapies that modulate their activity and for advancing our knowledge of how they contribute to various physiological and pathological processes in the body.
(-)-Nicotine ditartrate is a potent agonist of AChR (nicotinic acetylcholine recepto).
Synonyms: LY-2219620
LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.
Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors.
Synonyms: AF102B
Cevimeline (AF-102B) is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
Synonyms: Rivanicline; RJR 2403
Metanicotine is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than ??7 receptors(Ki= 36000 nM).
AC260584 is an M1 muscarinic receptor allosteric agonist with a pEC50 of 7.6.
Synonyms: LY246708
Xanomeline oxalate is a potent agonist of muscarinic acetylcholine receptors (EC50 values are 0.3, 92.5, 5, 52, and 42 nM for M1, M2, M3, M4, and M5, respectively).
TBPB is an allosteric M1 mAChR agonist with EC50 value of 89 nM that regulates amyloid processing and produces antipsychotic-like activity in rats.
Nitenpyram is a nicotinic acetylcholine receptor (AchR) agonist.
Synonyms: Evoxac
Cevimeline hydrochloride hemihydrate, a novel muscarinic receptor agonist, is a candidate therapeutic drug for xerostomia in Sjogren's syndrome.
Synonyms: Pilocarpine HCl; NSC 5746 HCl; (+)-Pilocarpine hydrochloride
Pilocarpine Hydrochloride is a selective agonist for the M3 muscarinic acetylcholine receptor (mAChR). It plays a significant role in stimulating glandular secretion, particularly in the treatment of dry mouth and glaucoma. This compound is valuable in research focused on neuropharmacology, as well as studies investigating cholinergic signaling and its implications in various physiological processes.
Synonyms: Acetyl-beta-methylcholine chloride; Provocholine; Mecholyl chloride; Amechol; Methapharma Brand of Methacholine Chloride; Provokit; Roche Brand of Methacholine Chloride
Methacholine chloride is a synthetic choline ester that acts as a non-selective muscarinic receptor agonist in the parasympathetic nervous system.
Synonyms: Evoxac; Cevimeline HCl
Cevimeline (Evoxac) Hcl is a parasympathomimetic and muscarinic agonist, with particular effect on M3 receptors; used in the treatment of dry mouth associated with sjogren's syndrome.
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.
Synonyms: Lu 25-109
Alvameline (Lu25-109) is a partial M1 agonist and M2/M3 antagonist.
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist(EC50=1.7 nM).
Synonyms: AE-37; AVex-73; Anavex-2-73
Blarcamesine, also known as AVex-73 and AE-37, is a muscarinic M1 agonist potentially for the treatment of Alzheimer's disease. It is an ς receptor ligand.
Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist.
Perlapine is a potent and selective hM3Dq DREADD agonist (EC50 = 2.8 nM). This drug exhibits >10,000-fold selectivity for hM3Dq over hM3.
VU0364572 TFA is a selective allosteric agonist of the M1 muscarinic receptor, exhibiting an EC50 of 0.11 μM. This compound demonstrates neuroprotective properties, making it a potential candidate for mitigating memory impairments and alleviating neuropathology associated with Alzheimer's Disease. Additionally, VU0364572 TFA is capable of penetrating the central nervous system, thus enabling its application in neurological research.
VU0364572 is a selective allosteric agonist of the M1 muscarinic receptor, exhibiting an EC50 of 0.11 μM. It demonstrates neuroprotective effects, making it a valuable tool in investigating memory impairments and neuropathological changes associated with Alzheimer’s Disease. Additionally, VU0364572 is orally bioactive and capable of penetrating the central nervous system, enhancing its utility in neuropharmacological research.
Clozapine N-oxide dihydrochloride is a selective agonist for designer receptors exclusively activated by designer drugs (DREADDs), specifically targeting hM3Dq and hM4Di. This compound plays a crucial role in neuronal circuit manipulation for experimental purposes. It is notable for its inability to cross the blood-brain barrier, making it useful for in vivo studies to modulate neuronal activity without central nervous system effects. Clozapine N-oxide dihydrochloride is integral in research applications related to neuroscience, enabling the dissection of gene function and behavior in animal models.
Synonyms: SB-202026 hydrochloride; Memric hydrochloride
Sabcomeline hydrochloride is a muscarinic receptor agonist with the ability to penetrate the blood-brain barrier. It exhibits strong affinity for human muscarinic receptor subtypes hM1 to hM5 (pKi=6.72-7.23) and functions as a near-full agonist at the hM3 receptor, leading to extracellular acidification. This compound also influences dopamine D2 receptor binding kinetics via neural network modulation, while exhibiting minimal effects on cardiovascular parameters. Sabcomeline hydrochloride is valuable in research related to Alzheimer's disease and other neurodegenerative disorders, especially for investigating its effects on spatial memory and taste aversion in rodent models.
Betovumeline hydrochloride is an agonist of muscarinic acetylcholine receptors (mAChRs), which play a critical role in various neurological functions. This compound is valuable for research into neurological disorders, facilitating the study of receptor activation and signaling pathways. Its ability to selectively engage mAChRs makes it a useful tool in pharmacological investigations and potential therapeutic applications.
Synonyms: LY-246708
Xanomeline is a selective agonist of the muscarinic M1 and M4 receptors, known to enhance neuronal excitability. This compound is primarily used in research focused on neurological disorders, including schizophrenia, and offers potential insights into the modulation of cholinergic signaling pathways in the central nervous system.