ノミフェンシン 化学特性,用途語,生産方法
説明
Nomifensine is an inhibitor of norepinephrine (NE) and dopamine (DA) reuptake. It inhibits uptake of NE, DA, and serotonin (5-HT) in rat brain synaptosomes with IC
50 values of 6.6, 48, and 830 nM, respectively. It is selective for DA, NE, and 5-HT uptake inhibition over binding to dopamine D
2, α
1- adrenergic-, 5-HT
2, and muscarinic receptors (IC
50s = 43,000, 1,200, 3,800, and >13,000 nM, respectively, in rat brain membranes). Nomifensine is selective for inhibition of NE over DA uptake
in vivo with minimal inhibitory doses of 28 and less than 57 μmol/kg, respectively. It decreases the time Wistar Kyoto, but not Sprague-Dawley, rats spend immobile in the forced swim test but also increases locomotor activity in the open field test in Wistar Kyoto and Sprague-Dawley rats when administered at a chronic dose of 10 mg/kg.
使用
A novel antidepressant distinguished from existing tricyclic and tetracyclic antidepressants by its bicyclic structure.
定義
ChEBI: An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively.
世界保健機関（WHO）
Nomifensine, an antidepressant indicated for the treatment of a
wide range of depressive illness, was introduced in 1976. Subsequently rare cases
of haemolytic anaemia - sometimes fatal - thrombocytopenia, hepatotoxicity and
fever were associated with the use of the drug. Following discussions with
regulatory authorities in the United Kingdom and the Federal Republic of Germany
the major manufacturer withdrew all preparations containing nomifensine
worldwide in January 1986.
安全性プロファイル
Poison by ingestion andintravenous routes. Human systemic effects by ingestion:diffuse hepatitis, hemorrhage and decrease in the numberof blood platelets (thrombocytopenia). When heated todecomposition it emits toxic fumes of NOx.
ノミフェンシン 上流と下流の製品情報
原材料
準備製品