mAChR

Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.

Imidafenacin is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).

Piperidolate hydrochloride is an antimuscarinic, Also a potential inhibitor of human glutathione transferase P1-1.

Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.

Piperidolate is a tertiary amine antimuscarinic. It is similar to atropine. It is mainly used in the smooth muscle spasm of the gastrointestinal tract and inhibits intestinal cramp induced by acetylcholine in rats and dogs.

Levetimide is a potent and stereoselective inhibitor of [3H](+)pentazocine binding, with a Ki of 2.2 nM.

Flavoxate hydrochloride is a competitive inhibitor of phosphodiesterase (PDE), providing significant antispasmodic effects through its action as a muscarinic acetylcholine receptor (mAChR) antagonist. In addition to its PDE inhibition, it exhibits moderate calcium antagonistic properties and local anesthetic effects. Flavoxate hydrochloride is utilized in research focused on overactive bladder (OAB) and related lower urinary tract infections, contributing to a better understanding of these conditions and potential therapeutic approaches.

Tematropium is a selective muscarinic acetylcholine receptor (mAChR) inhibitor known for its soft anticholinergic properties. It demonstrates significant biological activity in modulating bronchoconstriction and respiratory secretions. Tematropium is commonly used in research focused on respiratory diseases, exploring its potential in the treatment of asthma and chronic obstructive pulmonary disease (COPD).

Timepidium bromide is a muscarinic acetylcholine receptor (mAChR) inhibitor that exhibits anticholinergic properties. It is primarily utilized in research investigating acetylcholine signaling pathways and the role of mAChR in various physiological and pathological processes. This compound is valuable for studying conditions influenced by cholinergic activity, including respiratory and gastrointestinal disorders.

(-)-Vesamicol is a vesicular acetylcholine transporter inhibitor that exerts its action by reversibly and non-competitively inhibiting the transport of acetylcholine into synaptic vesicles. This compound effectively blocks the activity of vesicular acetylcholine transporters in medial amygdala neurons, making it a valuable tool for studies related to neurotransmission and neurodevelopmental disorders. Its specific application is in research focused on central precocious puberty, providing insights into the role of acetylcholine transport in this condition.

Arborine is a potent mAChR inhibitor that modulates the peripheral actions of acetylcholine, leading to a significant reduction in blood pressure. This compound is particularly valuable in research applications focused on cardiovascular physiology and the mechanistic study of cholinergic signaling pathways. Its ability to influence blood pressure dynamics makes it an important tool for investigating therapeutic interventions in hypertension and related disorders.

VU6008055 is a potent, selective allosteric modulator targeting the M4 muscarinic acetylcholine receptor, with EC50 values of 73.4 nM for human M4 and 19.5 nM for rat M4. This compound is capable of crossing the blood-brain barrier and exhibits oral bioactivity, making it a valuable tool for neuropharmacological research. VU6008055 demonstrates antipsychotic-like effects, contributing to its potential applications in studying psychiatric disorders and related therapeutic approaches.

(Rac)-Sabcomeline hydrochloride is a selective agonist of the M1 muscarinic acetylcholine receptor (mAChR). It exhibits potential neuroprotective effects and is of significant interest in research related to Alzheimer's disease and cognitive disorders. This compound is utilized in studies aimed at understanding the role of muscarinic receptors in synaptic plasticity and memory function.

BTM-1042 is a selective muscarinic acetylcholine receptor (mAChR) inhibitor with notable antispasmodic properties. It effectively inhibits electrical stimulation-induced contraction in the guinea pig ileum and demonstrates a dose-dependent reduction in spontaneous movement of the rabbit stomach. BTM-1042 displays similar activity to atropine in blocking muscarinic receptors while having a minimal impact on other receptor types. Additionally, it suppresses ileal responses triggered by nicotine and 5-hydroxytryptamine, highlighting its potential utility in gastrointestinal research applications and studies related to smooth muscle contraction modulation.

FK 584 is a potent detrusor muscle contraction inhibitor that primarily exhibits antimuscarinic activity alongside weak calcium channel blocking properties. This compound has shown significant efficacy in inhibiting detrusor muscle contractions across various experimental models, making it a valuable tool for research on overactive bladder (OAB). FK 584 presents a manageable risk of mydriasis, enabling detailed exploration of its therapeutic potential in bladder function studies.

(S)-Tolterodine is a selective muscarinic acetylcholine receptor (mAChR) inhibitor, exhibiting an IC50 value of 588 nM. This compound is primarily used in studies related to bladder overactivity and other cholinergic signaling pathways. Its pharmacological properties make it a valuable tool for investigating the mechanisms of mAChR modulation in both clinical and preclinical research.

Phenglutarimid hydrochloride is identified as a muscarinic acetylcholine receptor (mAChR) inhibitor. This compound exhibits anticholinergic properties and is primarily utilized in research related to Parkinson's disease and other neurological disorders. Its ability to modulate cholinergic signaling makes it a valuable tool for investigating therapeutic approaches for movement disorders and cognitive function.

Heliosupine N-oxide is a potent inhibitor of muscarinic acetylcholine receptors (mAChR), exhibiting an IC50 value of 350 μM. As a metabolite of Heliosupine and classified as a pyrrolizidine alkaloid, Heliosupine N-oxide serves as a valuable tool for research into cholinergic signaling pathways and related neurological studies. Its inhibitory properties can aid in elucidating the role of mAChR in various physiological and pathological processes.

Phenglutarimid is a muscarinic acetylcholine receptor (mAChR) inhibitor that exhibits anticholinergic properties. It is primarily utilized in research related to Parkinson's disease and other cholinergic dysfunctions. Its ability to modulate neurotransmitter activity makes it a valuable tool for investigating the therapeutic mechanisms underlying movement disorders.

Imidafenacin hydrochloride is an orally active inhibitor of muscarinic M1 and M3 receptors. It effectively inhibits bladder contraction in vivo, demonstrating significant antidiuretic effects through the enhancement of vasopressin signaling. This compound is particularly relevant for research focused on overactive bladder and related conditions, making it a valuable tool in the study of urinary disorders.

Cyclobuxine D is a steroidal alkaloid that functions as a muscarinic acetylcholine receptor (mAChR) inhibitor. It exhibits a notable bradycardic effect in rat models and effectively inhibits contractions induced by acetylcholine and Ba++ in isolated rabbit jejunum muscle. Due to its biological activities, Cyclobuxine D is valuable for research in pharmacology and cardiovascular studies.

ONO 1603 is a selective inhibitor of prolyl endopeptidase (PREP), investigated for its potential in antidementia therapy. This compound has demonstrated neuroprotective properties and neurotrophic effects in cerebellar granule cells, enhancing neuronal survival and promoting neurite outgrowth at a concentration of 0.03 µM. Additionally, ONO 1603 increases m3-muscarinic acetylcholine receptor (mAChR) mRNA levels and stimulates mAChR-mediated signaling pathways. These pharmacological properties suggest that ONO 1603 could be a promising therapeutic agent for Alzheimer's disease by enhancing cholinergic neurotransmission and supporting neuronal function.

Methylbenactyzium Bromide is a selective inhibitor of muscarinic acetylcholine receptors (mAChR). This compound effectively modulates cholinergic signaling pathways and is utilized in research focused on neuropharmacology, cardiovascular physiology, and respiratory function. Its ability to inhibit mAChR activity makes it a valuable tool in studies investigating the role of acetylcholine in various physiological processes and disease states.

Otilonium bromide is a selective inhibitor of muscarinic acetylcholine receptors (mAChR) with pronounced smooth muscle relaxant properties. This compound primarily functions by modulating calcium mobilization in intestinal smooth muscle, making it a valuable tool in the study of gastrointestinal disorders. Otilonium bromide is widely utilized in research related to irritable bowel syndrome and other smooth muscle-related conditions.

Camylofine is an antimuscarinic compound that selectively inhibits muscarinic acetylcholine receptors (mAChRs). It functions as a smooth muscle relaxant, making it useful in various research applications related to muscle contraction and neurotransmission. This compound is valuable for studying the physiological effects of cholinergic signaling and exploring potential therapeutic interventions for conditions related to smooth muscle hyperactivity.

Tolterodine is an mAChR inhibitor that competitively binds to acetylcholine, leading to a reduction in sympathetic excitation and inhibition of involuntary bladder muscle contractions. It is known to restore the Nrf2/NF-κB signaling pathway, providing protection against inflammatory responses and ferroptosis. Additionally, Tolterodine mitigates LPS-induced reactive oxygen species production and lipid oxidation, making it valuable for research in urinary tract infections and overactive bladder conditions.

Trospium chloride is a selective and competitive antagonist of muscarinic acetylcholine receptors (mAChRs). It exhibits potent antimuscarinic activity by binding with high affinity to M1, M2, and M3 receptor subtypes, while showing no interaction with nicotinic cholinergic receptors. This compound is primarily utilized in research related to neurological conditions and to explore the pharmacological modulation of cholinergic signaling.