4-アミノピリジン 化学特性,用途語,生産方法
外観
白色～赤褐色, 結晶～結晶性粉末
溶解性
水に易溶, エタノール, エーテルに可溶。水、エタノール及びアセトンに溶けやすい。
用途
有機合成原料(医薬、農薬)。
用途
鳥よけ、駆除剤の中間体
効能
けいれん誘発薬, カリウムチャネル遮断薬
説明
4-Aminopyridine (4-AP, fampridine, dalfampridine) is the first drug approved by the FDA to improve walking in patients with multiple sclerosis (MS). Dalfampridine is a voltage-gated potassium channel blocker that readily penetrates the CNS and increases the conduction and duration of action potential across nerve fibers resulting in enhanced functionality as observed in the walking speed of MS patients.
From a safety perspective, seizure was the most important adverse event from various dalfampridine clinical trials. Therefore, dalfampridine is contraindicated in patients with a history of seizures. Since dalfampridine is primarily excreted by the kidney as unchanged drug, it is also contraindicated in patients with moderate to severe renal impairment. Assessing the overall benefit–risk profile from various clinical trials, the FDA approved dalfampridine (daily oral dose of 10 mg, b.i.d.) to improve walking in MS patients with existing gait impairment.
化学的特性
4-aminopyridine is a white crystalline solid that contains about 98% active ingredient. It is soluble in water and slightly soluble in benzene and ether. 4-Aminopyridine formulations are classifi ed by the US Environmental Protection Agency (US EPA) as restricted
use pesticides (RUPs) and therefore should be purchased and used only by certifi ed and
trained workers and applicators. Avitrol is available as grain baits or as a powder concentrate. It is one of the most prominent avicides. It is registered with the EPA for use against
red-winged blackbirds, blackbirds in agricultural fi elds, grackles, pigeons, and sparrows
around public buildings, and various birds around livestock feeding pens. Avitrol repels
birds by poisoning a few members of a fl ock, causing them to become hyperactive.
使用
Avitrol (4-aminopyridine), has repellent–toxicant properties for birds and is classed as a severe poison and irritant. This secondary bird repellent can be used as a broadcast bait, causing uncoordinated flight and distress calls and escape responses in nearby birds.
定義
ChEBI: 4-aminopyridine is an aromatic amine that is pyridine bearing a single amino substituent at position 4. An orphan drug in the US, it is used to improve walking in adults with multiple sclerosis. It has a role as an avicide, a potassium channel blocker and an orphan drug. It is an aromatic amine and an aminopyridine.
一般的な説明
White crystalline material with no odor. Used as an avicide, an intermediate and as a fixer for some textile dyes.
反応プロフィール
4-Aminopyridine neutralizes acids in exothermic reactions to form salts plus water. 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
4-Aminopyridine, a pyridine compound, is an extremely effective bird poison. In agriculture, 4-AP is used as an extremely effective bird poison sold under the brand name Avitrol. It is highly toxic to all mammals including humans if dosages are exceeded, and as an experimental drug, the recommended dose data is unavailable.
火災危険
Material may produce irritating or poisonous gases in fire. Runoff from fire control water may give off irritating or poisonous gases.
安全性プロファイル
Poison by ingestion, subcutaneous, intravenous, and intraperitoneal routes. Human systemic effects by ingestion: hallucinations and vomiting. When heated to decomposition it emits toxic fumes of NOx,.
職業ばく露
Used as a chemical intermediate in pharmaceuticals; as an agricultural chemical for field crops; and as a bird repellent and poison
輸送方法
UN2671 Aminopyridines, Hazard Class: 6.1; Labels: 6.1-Poisonous materials
純化方法
Crystallise the aminopyridine from *benzene/EtOH, then recrystallise it twice from water, then crush and dry it for 4hours at 105o [Bates & Hetzer J Res Nat Bur Stand 64A 427 1960]. It has also been crystallised from EtOH, *benzene, *benzene/pet ether, toluene and sublimes in a vacuum. [Beilstein 22/9 V 106.]
不和合性
Sodium nitrite, strong oxidizers. Avoid contact with acid anhydrides, acid chlorides; and strong acids.
廃棄物の処理
Consult with environmental regulatory agencies for guidance on acceptable disposal practices. Generators of waste containing this contaminant (≥100 kg/mo) must conform with EPA regulations governing storage, transportation, treatment, and waste disposalIncineration with nitrogen oxides removal from effluent gas.
4-アミノピリジン 上流と下流の製品情報
原材料
準備製品