臭化クリジニウム 化学特性,用途語,生産方法
効能
ムスカリン受容体拮抗薬
説明
Clidinium is a gastrointestinal muscarinic receptor antagonist (K
i = 3 nM against [
3H]quinuclidinyl benzilate binding in rat colonic enterocytes). Administration of clidinium, at a dose of 1 mg/kg, slows intestinal transit and induces constipation in mice. This clidinium-induced constipation induces serum hyperammonemia and decreases clonic, myoclonic, and tonic seizure thresholds in a murine pentylenetetrazole-induced epilepsy model.
化学的特性
White Crystalline Solid
使用
Clidinium inhibits muscarinic action of acetylcholine on postganglionic parasympathetic
effector regions. It is used for treating stomach ulcers.
定義
ChEBI: The bromide salt of clinidium. It is used for the symptomatic treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome.
一般的な説明
Clidinium bromide, 3-hydroxy-1-methylquinuclidinium bromide benzilate (Quarzan),is a white or nearly white, almost odorless, crystalline powderthat is optically inactive. It is soluble in water and alcohol butonly very slightly soluble in ether and benzene.
臨床応用
This anticholinergic agent is marketed alone and in combinationwith the minor tranquilizer chlordiazepoxide (Librium)in a product known as Librax. The rationale of the combinationfor the treatment of GI complaints is the use of an anxiety-reducing agent together with an anticholinergic agent,based on the recognized contribution of anxiety to the developmentof the diseased condition. It is suggested for pepticulcer, hyperchlorhydria, ulcerative or spastic colon, anxietystates with GI manifestations, nervous stomach, irritable orspastic colon, and others. Clidinium bromide is contraindicatedin glaucoma and other conditions that may be aggravatedby the parasympatholytic action, such as prostatic hypertrophyin elderly men, which could lead to urinary retention.
合成
Clidinium, 3-benzyloyloxy-1-methylcynuclidinium bromide (14.1.19), is
synthesized by reacting 3-hydroxycynuclidine (14.1.17) with the of benzilic acid chloride
producing the ester (14.1.18), which if further alkylated at the nitrogen atom by methylbromide, giving clidinium (14.1.19) [16].
臭化クリジニウム 上流と下流の製品情報
原材料
準備製品