Scopolamine N-oxide hydrobromide is an antagonist of the muscarinic acetylcholine.
(R)-Oxybutynin (Aroxybutynin), a (R)-isomer of Oxybutynin, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin can be used for researching incontinence due to neurogenic bladder dysfunction[1][2][3].
Scopolamine hydrobromide is a high affinity (nM) muscarinic antagonist. 5-HT3 receptor-responses are reversibly inhibited by Scopolamine with an IC50 of 2.09 μM.
Homatropine Methylbromide is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.target： mAChRIC 50: WKY-E(162.5 nM), SHR-E(170.4nM )In vitro: Homatropine (20 μM) alone produces a dose ratio of 259 in atrium from guinea-pigs. Homatropine (20 μM) produces a dose ratio of only 95.0 when combined with hexamethonium in atrium from guinea-pigs.In vivo: : Pre-treatment with homatropine (20 mg/kg) was comparable with atropine (10 mg/kg) in preventing lethality in this rat model of acute OC poisoning. All rats pre-treated with normal saline, atropine 5 mg/kg, and homatropine 10 mg/kg died. Survival in the homatropine (20 mg/kg) and atropine (10 mg/kg) groups was 30% and 40% respectively.
Sabcomeline (SB-202026) is a potent and functionally selective muscarinic M1 receptor partial agonist that improve cognition. Sabcomeline can be used for Alzheimer's disease research[1][2].
Elucaine is a muscarinic acetylcholine receptor antagonist with anti-ulcerative activity.
Anisodamine is an anticholinergic and α1-adrenergic receptor antagonist used in the treatment of acute circulatory shock, is also a naturally occurring tropane alkaloid found in some plants of the Solanaceae family.
Procyclidine (Tricyclamol; (±)-Procyclidine), an anticholinergic agent, is a muscarinic receptor antagonist that also has the properties of an N-methyl-D-aspartate (NMDA) antagonist. Procyclidine can be used in studies of Parkinson's disease and related psychiatric disorders such as Soman-induced epilepsy[1][2].
Scopolamine butylbromide is a competitive antagonist of muscarinic acetylcholine receptor (mAChR) with an IC50 of 55.3 ± 4.3 nM.Target: mAChRScopolamine (USAN), also known as levo-duboisine and hyoscine, sold as Scopoderm, is a tropane alkaloid drug with muscarinic antagonist effects. It is among the secondary metabolites of plants from Solanaceae (nightshade) family of plants, such as henbane, jimson weed (Datura), angel's trumpets (Brugmansia), and corkwood (Duboisia). Scopolamine exerts its effects by acting as a competitive antagonist at muscarinic acetylcholine receptors, specifically M1 receptors; it is thus classified as an anticholinergic, antimuscarinic drug. Its use in medicine is relatively limited, with its chief uses being in the treatment of motion sickness and postoperative nausea and vomiting. Scopolamine is named after the plant genus Scopolia. The name "hyoscine" is from the scientific name for henbane, Hyoscyamus niger.
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. Used in the research of neuropsychiatric disorders[1].
CDDD3602 is a soft anticholinergics.
Milameline is a muscarinic receptor agonist that improves cognition.
Penehyclidine (Penequinine) hydrochloride, a anticholinergic drug, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation[1].
Navafenterol (AZD-8871) saccharinate is an inhaled dual-acting, potent, selective, and long-lasting M3-antagonist/β2-agonist (MABA) with long-lasting effects and favorable safety profile. The pIC50 is 9.5 for human M3 receptor, and the pEC50 is 9.5 for β2-adrenoceptor. Navafenterol saccharinate can be used for the research of chronic obstructive pulmonary disease (COPD). Bronchoprotective and antisialagogue effects. Favorable cardiovascular profile[1].
Atropine methyl bromide, a muscarinic receptor (mAChR) antagonist, is a quaternary ammonium salt of atropine and a mydriatic for dilation of the pupil during ophthalmic examination. It is introduced for relieving pyloric spasm in infants for its highly polar nature. It penetrates less readily into the central nervous system than atropine[1][2].
Rispenzepine is a novel antimuscarinic compound with a preferential action at M1, and M3 receptor subtypes.
(R)-Oxybutynin hydrochloride, a (R)-isomer of Oxybutynin hydrochloride, is an orally active muscarinic receptor antagonist. (R)-Oxybutynin hydrochloride has antimuscarinic, antispasmodic and anticholinergic activity, competitively antagonizes Carbachol-induced contractions. (R)-Oxybutynin hydrochloride can be used for researching incontinence due to neurogenic bladder dysfunction[1][2][3].
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively[1].
Cyclopentolate (DL-Cyclopentolate) is an Atropine-like muscarinic receptors antagonist with a pKB value of 7.8 (on the circular ciliary muscle). Cyclopentolate is an anti-muscarinic agent commonly used in the ophthalmologic practice[1][2].
Muscarine ((+)-Muscarine) is a toxin that can stimulate the parasympathetic nervous system. Muscarine is an agonist of muscarinic acetylcholine receptor (mAChR)[1][2].
(R)-5-Hydroxymethyl Tolterodine(PNU-200577; Desfesoterodine) is a potent and selective muscarinic receptor antagonist with a Kb and a pA2 of 0.84 nM and 9.14, respectively. IC50 value: 0.84 nM (Kb)Target: mAChR(R)-5-Hydroxymethyl Tolterodine is a major pharmacologically active metabolite of tolterodine. In vitro, (R)-5-Hydroxymethyl Tolterodine prevented carbachol-induced contraction of guinea-pig isolated urinary bladder strips in a competitive and concentration-dependent manner. In vivo, (R)-5-Hydroxymethyl Tolterodine was significantly more potent at suppressing acetylcholine-induced urinary bladder contraction than electrically induced salivation in the anaesthetised cat (ID50=15 and 40 nmol/kg, respectively). In radioligand binding studies carried out in homogenates of guinea-pig tissues and Chinese hamster ovary cell lines expressing human muscarinic m1-m5 receptors, (R)-5-Hydroxymethyl Tolterodine was not selective for any muscarinic receptor subtype. Thus, (R)-5-Hydroxymethyl Tolterodine is similar to tolterodine in terms of antimuscarinic potency, functional selectivity for the urinary bladder in vivo and absence of selectivity for muscarinic receptor subtypes in vitro. The results of this study clearly indicate that (R)-5-Hydroxymethyl Tolterodine contributes to the therapeutic action of tolterodine, in view of its high antimuscarinic potency, similar serum concentration and lower degree of protein binding.
N-Desethyloxybutynin hydrochloride is an active metabolite of Oxybutynin. N-Desethyloxybutynin hydrochloride binds to mAChRs in isolated? human bladder and human parotid gland with pKi values of 8.2 and 8.7, respectively[1].
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively[1][2].
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[1]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[2].
Tropicamide-d3 is the deuterium labeled Tropicamide[1]. Tropicamide (Ro 1-7683) is a selective M4 muscarinic acetylcholine receptor antagonist. Tropicamide produces short acting mydriasis (dilation of the pupil) and cycloplegia when applied as eye drops[2][3].
Homatropine is an orally active muscarinic acetylcholine receptor antagonist and can be used as an anticholinergic agent[1].
Carbamoylcholine chloride is used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.IC50 value: 10 to 10,000 nM (Ki)Target: nAChR, mAChRCarbamoylcholine is an analog of acetylcholine that activates acetylcholine receptors (AChR). Carbamoylcholine is an agonist of both nicotinic (nAChR) and muscarinic (mAChR) receptors, with reported Ki values ranging from 10 to 10,000 nM for different receptors and different preparations.
Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist[1][2].
Zamifenacin (UK-76654) is a potent gut-selective muscarinic M3 receptor antagonist. Zamifenacin significantly reduces colonic motility in irritable bowel syndrome[1].
Biperiden(KL 373) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker.Target: M1 receptorsBiperiden is an antiparkinsonian agent of the anticholinergic type. It is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arteriosclerotic)[1]. Biperiden has an atropine-like blocking effect on all peripheral structures which are parasympathetic-innervate. It also has a prominent central blocking effect on M1 receptors [2].Biperiden (0.11 mg/kg), benactyzine (0.3 mg/kg),caramiphen (10 mg/kg), procyclidine (3 mg/kg), and trihexyphenidyl (0.12 mg/kg) separately and each in combination with physostigmine (0.1 mg/kg) is to make a comparative assessment of potential cognitive effects. The results showed that benactyzine, caramiphen, and trihexyphenidyl reduced rats' innate preference for novelty, whereas biperiden and procyclidine did not [3].Clinical indications: parkinsonismFDA Approved Date: Toxicity: Drowsiness; vertigo; headache; dizziness