NOMIFENSINE MALEATE Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
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.
Verwenden
A novel antidepressant distinguished from existing tricyclic and tetracyclic antidepressants by its bicyclic structure.
Definition
ChEBI: An N-methylated tetrahydroisoquinoline carrying phenyl and amino substituents at positions C-4 and C-8, respectively.
Weltgesundheitsorganisation (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.
Sicherheitsprofil
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.
NOMIFENSINE MALEATE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
