T71236
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Oxybutynin R-isomer , also known as Aroxybutynin, is a muscarinic receptor antagonist. Aroxybutynin is the optically avtice inhibitor of proliferation and supresses gene expression in bladder smooth muscle cells. Oxybutynin exerts direct antispasmodic effect on smooth muscle and inhibits the muscarinic action of acetylcholine on smooth muscle. It exhibits one-fifth of the anticholinergic activity of atropine on the rabbit detrusor muscle, but four to ten times the antispasmodic activity. No blocking effects occur at skeletal neuromuscular junctions or autonomic ganglia (antinicotinic effects). |
T60578
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Procyclidine (Tricyclamol; (±)-Procyclidine) 是一种抗胆碱能剂。它是一种毒蕈碱受体 (muscarinic receptor) 拮抗剂,也是 N-甲基-D-天冬氨酸 (NMDA) 拮抗剂。Procyclidine 可用于帕金森症和相关精神疾病的研究,如Soman 诱发的癫痫。 |
T69119
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Disopyramide HCl is the salt form of Disopyramide, an antiarrhythmic medication used in the treatment of ventricular tachycardia. It is a sodium channel blocker and therefore classified as a Class 1a anti-arrhythmic agent. Disopyramide has a negative inotropic effect on the ventricular myocardium, significantly decreasing the contractility. Disopyramide also has an anticholinergic effect on the heart which accounts for many adverse side effects. Disopyramide is available in both oral and intravenous forms, and has a low degree of toxicity. |
T75691
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Amaroswerin为从獐牙菜提取的硫环烯醚萜苷,显示出抗炎、抗糖尿病、抗病毒、抗胆碱能及免疫调节生物活性。在RAW264.7细胞模型中,Amaroswerin能够抑制NO的释放,其IC50值达到5.42 μg/mL。 |
T60843
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Brompheniramine ((±)-Brompheniramine) 是具有口服活性的烷基胺类抗组胺药。Brompheniramine 是组胺 H1 受体的选择性拮抗剂 (Kd = 6.06 nM)。Brompheniramine 可用于过敏性鼻炎,它具有抗胆碱能、抗抑郁和麻醉作用。Brompheniramine 可阻断钙离子通道、钠离子通道和 hERG 通道,IC50分别为 16.12 μM, 21.26 μM 和 0.90 μM。 |
T60428
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Cibenzoline 是一种抗心律失常药,通过直接影响成孔 Kir6.2 亚基而不是 SUR1 亚基来抑制 KATP 通道。 Cibenzoline 几乎不具有抗胆碱能活性。 Cibenzoline 显着降低与心肌收缩力下降密切相关的LVPG。 Cibenzoline 具有研究肥厚型梗阻性心肌病的潜力[1][2]。 |
T70070
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Cisapride tartrate is chemically related to metoclopramide, but unlike metoclopramide, it does not cross the blood-brain barrier or have antidopaminergic effects. Cisapride is a serotonin-4 (5-HT4) receptor agonist. Cisapride was indicated for the symptomatic treatment of adult patients with nocturnal heartburn due to gastroesophageal reflux disease. The Food and Drug Administration (FDA) in America stopped the marketing of cisapride as of 14th July 2000. They had received at least 341 reports of heart rhythm abnormalities and these led to 80 deaths. Other reported adverse effects are: headache, diarrhea, abdominal pain, nausea, constipation. Cisapride for animals has been found helpful in some cases of megaesophagus and is a common treatment for feline megacolon. Clarithromycin, erythromycin, and troleandomycin markedly inhibit the metabolism of cisapride. Concurrent administration of certain anticholinergic compounds, such as belladonna alkaloids and dicyclomine, would be e...... |
T14614
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Others
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Biperiden Hydrochloride (KL 373 Hydrochloride) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker and it is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arte |
T36204
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Methylatropine is an antagonist of muscarinic acetylcholine receptors (IC50= <0.1 nM in a radioligand binding assay using isolated porcine brain membranes) and a derivative of atropine .1,2It reduces acetylcholine-induced decreases in blood pressure in rats when administered intravenously with an ED50value of 5.5 μg/kg.2Methylatropine reduces salivation, induces mydriasis, and increases heart rate in dogs.3
1.Schmeller, T., Sporer, F., Sauerwein, M., et al.Binding of tropane alkaloids to nicotinic and muscarinic acetylcholine receptorsPharmazie50(7)493-495(1995) 2.Brezenoff, H.E., Xiao, Y.-F., and Vargas, H.A comparison of the central and peripheral antimuscarinic effects of atropine and methylatropine injected systemically and into the cerebral ventriclesLife Sci.42(8)905-911(1988) 3.Albanus, L.Central and peripheral effects of anticholinergic compoundsActa Pharmacol. Toxicol. (Copenh)28(4)305-326(1970) |