Naftopidil dihydrochloride

Bezeichnung:Naftopidil dihydrochloride

Englisch Name:Naftopidil dihydrochloride

CBNumberCB6356910

SummenformelC24H28N2O3

Molgewicht392.49

Naftopidil dihydrochloride physikalisch-chemischer Eigenschaften

Schmelzpunkt	127 °C
Siedepunkt	517.2°C (rough estimate)
Dichte	1.1592 (rough estimate)
Brechungsindex	1.6300 (estimate)
storage temp.	Sealed in dry,Room Temperature
Löslichkeit	methanol: >10 mg/mL
Aggregatzustand	solid
pka	14.01±0.20(Predicted)
Farbe	white
Merck	14,6356
CAS Datenbank	57149-07-2(CAS DataBase Reference)

Sicherheit

RIDADR	3077
WGK Germany	3
RTECS-Nr.	TL9336500
HS Code	29335990
Toxizität	LD50 in mice, rats (g/kg): 1.3, 6.4 orally (Himmel)

Gefahreninformationscode (GHS)

Beschreibung
Naftopidil was launched in Japan for the treatment of dysuria associated with benign prostatic hypertrophy (BPH). It can be prepared by a two step route starting with α-naphthol. Naftopidil is a potent postsynaptic-selective alpha-l-antagonist with a slightly higher affinity for the human prostatic than for the aortic alpha-adrenoceptor. It also shows a 5-HT1A agonistic effect, as well as a weak calcium antagonistic activity, but no alpha-2 or beta-adrenoreceptor affinity. In experiments with rats or rabbits, Naftopidil was shown to be more potent and selective for the urodynamic effect than the hypotensive effect. Aromatic or aliphatic hydroxylation are the major routes of metabolism, producing metabolites with a profile similar to the parent compound.
Chemische Eigenschaften
Off-White Solid
Originator
Boehringer Mannheim (Germany)
Verwenden
A α-1-Adrenergic receptor antagonist, antihypertensive.
Verwenden
Naftopidil is an α-1-adrenergic receptor antagonist. Naftopidil is used as an antihypertensive.
Verwenden
antihypertensive, alpha-blocker, 5HT1a agonist
Definition
ChEBI: Naftopidil is a member of piperazines.
Trademarks
Avishot;Flivas
Biologische Aktivität
An α 1 -adrenoceptor antagonist with only weak antagonism at post-junctional α 2 receptors; a potent, persistent antihypertensive and vasodilator.