デキストロメトルファン臭化水素酸塩一水和物

外観

白色, 結晶〜結晶性粉末

溶解性

メタノールに極めて溶けやすく、エタノールに溶けやすく、水にやや溶けにくい。

用途

薬理研究用。

効能

鎮咳薬

商品名

メジコン (塩野義製薬)

説明

Dextromethorphan (DXM) is a dextratrorotatory morphinan with structural similarity to levorphanol, codeine, and morphine. Because of its strong antitussive effects, dextromethorphan is widely used as a cough suppressant. However, it does not provoke opioid activity as is characteristic of several other morphine derivatives. DXM binds to and inhibits NMDA (IC₅₀ = 0.55 μM) and nicotinic receptors (IC₅₀s = 0.7-3.9 μM) and blocks receptor-gated and voltage-gated calcium channels (IC₅₀ = 60 μM) and voltage-gated sodium channels (IC₅₀ = 78 μM). DXM has been used in multimodal analgesic therapies for acute and neuropathic pain.

化学的特性

White Solid

使用

An antitussive drug. Orally active synthetic morphine analog. Analgesic (narcotic). Racemethorphan and levomethorpham are controlled substances (opiates).

生物活性

Non-competitive, low affinity NMDA receptor antagonist. Antitussive, anticonvulsive and neuroprotective agent.