- Cat. No.
- A12333
Darenzepine
Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.
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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.
Darenzepine is a muscarinic receptor inhibitor extracted from patent US 20170095465 A1.
Synonyms: KRP-197; ONO-8025
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).
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.
Synonyms: Rec-7-0040; DW61
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.
Synonyms: Octylonium bromide; SP63
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.
Synonyms: (R)-(+)-Tolterodine; (+)-Tolterodine; (R)-Tolterodine; PNU-200583
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.
Synonyms: Dactil; Crapinon; NSC 4349; Piperidolate HCl
Piperidolate hydrochloride is an antimuscarinic, Also a potential inhibitor of human glutathione transferase P1-1.
Synonyms: 6-Hydroxy hyoscyamine; 654-II
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
Synonyms: 1087 A.N.; BRN 0031110; Dactil; JB 305; Piperidolatum
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.
Synonyms: KL 373
Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.
Synonyms: Isothazine
Ethopropazine hydrochloride is a potent and selective inhibitor of butyrylcholinesterase (BChE) and acts as a non-selective antagonist at muscarinic acetylcholine receptors (mAChR) and N-methyl-D-aspartate receptors (NMDA). This compound exhibits anticholinergic, antihistamine, and antiadrenergic activities, making it valuable in studying its effects on neuropathic pain conditions such as thermal hyperalgesia. Ethopropazine hydrochloride is particularly relevant in research related to Parkinson's disease, providing insights into cholinergic system modulation and receptor interactions.
Synonyms: (-)-AH5183
(-)-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.
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.
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(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.
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Synonyms: Ciba 10870 hydrochloride; Phenglutarimide hydrochloride
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.
Synonyms: Ciba 10870; Phenglutarimide
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.
Synonyms: KRP-197 (hydrochloride); ONO-8025 (hydrochloride)
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.
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Mazaticol is an anticholinergic agent targeting muscarinic acetylcholine receptors. It effectively blocks cholinergic nerve activity and serves as a potent inhibitor of 3H-QNB and 3H-PZ binding, demonstrating high affinity for M2 receptors. Additionally, Mazaticol exhibits inhibitory effects on dopamine uptake in striatal nerve terminals, making it valuable for research into parkinsonian syndromes.
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.
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Synonyms: CDDD3602; HGP6
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).