マレイン酸ピリラミン 化学特性,用途語,生産方法
外観
白色〜ほとんど白色, 結晶〜粉末
溶解性
水、エタノール、アセトンに溶ける。
効能
抗アレルギー薬, H1受容体拮抗薬
説明
Mepyramine is a first generation antihistamine that acts as an inverse agonist at the histamine H
1 receptor. It is reported to bind with high affinity to a G
q/11 protein-coupled form of the receptor and to promote a G protein-coupled inactive state of the H
1 receptor that interferes with the G
q/11-mediated signaling of the endogenously expressed receptor, as well as to reduce G protein availability for other non-related receptors associated with this signaling pathway. Mepyramine has been shown to inhibit histamine-induced inositol phosphate production with a log EC
50 value of -7.94.
化学的特性
solid
使用
Pyrilamine maleate Selective inverse agonist for the H-1 histamine receptor. Pyrilamine Maleate is commonly utilized as a radioligand ([3H]Mepyramine) binding assay for the H1 receptor. And also used to exhibit blocking ability of KCNQ/M channels which is potentially related to an adverse effect seen in excess intake of antihistamines.
一般的な説明
White crystals or powder. Melting point 100-101°C. Bitter saline taste. An antihistaminic medicine.
空気と水の反応
Water soluble.
反応プロフィール
PYRILAMINE MALEATE is an acidic salt of an amine. Usually does not react as either oxidizing agents or reducing agents but such behavior is not impossible. May be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen may be generated in combination with strong reducing agents, such as hydrides.
健康ハザード
SYMPTOMS: Symptoms of exposure to PYRILAMINE MALEATE may include drowsiness, potentiation of the sedative effect of barbituates, fatigues, vertigo, incoordination, tremor, muscle weakness, dryness of the mouth and throat, tinnitus, pupillary dilation, blurred vision, urinary retention, impotence, epigastric and intestinal pain, anorexia, nausea, vomiting, diarrhea, excitation, euphoria, insomnia, nervousness, palpitation, tachycardia, hypotension, hypersensitivity reactions, respiratory depression, coma and delirium.
火災危険
Flash point data for PYRILAMINE MALEATE are not available, however PYRILAMINE MALEATE is probably combustible.
生物活性
Selective inverse agonist for the H 1 receptor. Inhibits histamine induced inositol phosphate (InsP) production (log EC50 = -7.94) and intracellular calcium mobilization. Sequesters G q/11 protein, reducing its availability for other receptors associated with the same signaling pathway.
安全性プロファイル
A human poison by
ingestion. An experimental poison by
ingestion, subcutaneous, intravenous, and
intraperitoneal routes. Experimental
reproductive effects. Questionable
carcinogen with experimental tumorigenic
data. Mutation data reported. An
antihistamine. When heated to
decomposition it emits toxic fumes of NOx.
マレイン酸ピリラミン 上流と下流の製品情報
原材料
準備製品