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Mirtazapine

Mirtazapine Struktur
61337-67-5
CAS-Nr.
61337-67-5
Englisch Name:
Mirtazapine
Synonyma:
ZISPIN;REMERON;ORG-3770;Remergon;Mirtazne;Mitazapine;MIRTAZEPINE;MIRTAZANINE;Mepirzepine;Mirtazapine
CBNumber:
CB7463387
Summenformel:
C17H19N3
Molgewicht:
265.35
MOL-Datei:
61337-67-5.mol

Mirtazapine Eigenschaften

Schmelzpunkt:
114-116°C
Flammpunkt:
9℃
storage temp. 
2-8°C
L?slichkeit
DMSO: ~8 mg/mL, soluble
Aggregatzustand
solid
pka
pKa 7.1(47% MeOH in H2O,t =25,I=0.15(KCl)) (Uncertain)
Farbe
white
CAS Datenbank
61337-67-5(CAS DataBase Reference)
NIST chemische Informationen
Mirtazapine(61337-67-5)
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Kennzeichnung gef?hrlicher F,T
R-S?tze: 11-23/24/25-39/23/24/25
S-S?tze: 22-24/25-45-36/37-16-7
RIDADR  UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany  3
Bildanzeige (GHS) GHS hazard pictogramsGHS hazard pictogramsGHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H225 Flüssigkeit und Dampf leicht entzündbar. Entzündbare Flüssigkeiten Kategorie 2 Achtung GHS hazard pictogramssrc="/GHS02.jpg" width="20" height="20" /> P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H370 Sch?digt die Organe. Spezifische Zielorgan-Toxizit?t (einmalige Exposition) Kategorie 1 Achtung GHS hazard pictogramssrc="/GHS08.jpg" width="20" height="20" /> P260, P264, P270, P307+P311, P321,P405, P501
Sicherheit
P210 Von Hitze, hei?en Oberfl?chen, Funken, offenen Flammen und anderen Zündquellenarten fernhalten. Nicht rauchen.
P260 Dampf/Aerosol/Nebel nicht einatmen.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P301+P310 BEI VERSCHLUCKEN: Sofort GIFTINFORMATIONSZENTRUM/Arzt/... (geeignete Stelle für medizinische Notfallversorgung vom Hersteller/Lieferanten anzugeben) anrufen.
P311 GIFTINFORMATIONSZENTRUM/Arzt anrufen.

Mirtazapine Chemische Eigenschaften,Einsatz,Produktion Methoden

S-S?tze Betriebsanweisung:

S22:Staub nicht einatmen.
S24/25:Berührung mit den Augen und der Haut vermeiden.

Beschreibung

Mirtazapine is an antidepressant launched in the Netherlands. Mirtazapine is a potent antagonist of presynaptic α2 receptors as well as a moderately potent 5-HT antagonist. Studies suggested that blockade of α2-adrenoceptors, but not inhibition of noradrenaline uptake, is involved in the mechanism of the antidepressant action of mirtazapine. Mirtazapine has demonstrated efficacy in various studies in depressed patients, being equal or more potent than mianserin, amitriptyline, etc. and exhibiting less anticholinergic and gastrointestinal side effects and low cardiovascular toxicity. In addition to its antidepressant effects, studies in animals indicated that mirtazapine has anxiolytic andor hypnotic activity.

Chemische Eigenschaften

White Crystalline Solid

Verwenden

An a 2-Adrenergic blocker. An analogue of Mianserin. Antidepressant

Biologische Funktion

Mirtazapine (Remeron) enhances both serotonergic and noradrenergic neurotransmission. By blocking presynaptic α2-adrenoceptors, mirtazapine causes release of norepinephrine. Indirectly, through noradrenergic modulation of serotonin systems, mirtazapine also causes increased release of serotonin. It is an antagonist at the 5-HT2A, 5HT2C, 5-HT3, and histamine receptors but has minimal affinity for muscarinic or α1-receptors. Mirtazapine does not inhibit neuronal reuptake of serotonin or norepinephrine.Weight gain and sedation are common side effects; sedation necessitates dosing at bedtime. Mirtazapine does not have significant effects on cytochrome P450 isoenzymes.

Allgemeine Beschreibung

Mirtazapine (Remeron) is another example of tetracyclicα2-blockers that shows selectivity for α2-receptorsversus 1-receptors. Blockade of central α2-receptors resultsin an increased release of NE and serotonin. This hasprompted its use as an antidepressant. This agent also hasactivity at nonadrenergic receptors. It is a potent blockerof 5-HT2 and 5-HT3 serotonin receptors and at histamineH1-receptors.

Mechanism of action

Animal studies indicate that the efficacy of mirtazapine as an antidepressant results from enhancing central noradrenergic and serotonergic activity, possibly through blocking central presynaptic α2-adrenergic receptors. Blocking these receptors inhibits the negative feedback loop, which increases the release of NE into the synapse. Mirtazapine also is a potent antagonist at 5-HT2 and 5-HT3 receptors, and it shows no significant affinity for 5-HT1A or 5-HT1B receptors. Additionally, it displays some anticholinergic properties, and it produces sedative effects (because of potent histamine H1 receptor antagonism) and orthostatic hypotension (because of moderate antagonism at peripheral α1-adrenergic receptors). Its antidepressant effect is comparable to the TCAs and may be better than some SSRIs, especially in patients with depression of the melancholic type, but at higher doses, it may cause drowsiness and weight gain. The drug generally is well tolerated, producing no more adverse events (including anticholinergic events) than the SSRIs and fewer adverse events than the TCAs.
Mirtazapine absorption is rapid and complete, with a bioavailability of approximately 50% as a result of first-pass metabolism. The rate and extent of mirtazapine absorption are minimally affected by food. Dose and plasma levels are linearly related over a dose range of 15 to 80 mg. The elimination half-life of the (–)-enantiomer is approximately twice that of the (+)-enantiomer. In females of all ages, the elimination half-life is significantly longer than in males (mean half-life, 37 versus 26 hours).

Clinical Use

Mirtazapine is a piperazinodibenzoazepine antidepressant that is an isostere of the antidepressant mianserin. A seemingly simple isosteric replacement of an aromatic methine group (CH) in mianserin with a nitrogen to give a pyridine ring (mirtazapine) has profound effects on the physicochemical properties, pharmacokinetics, mechanisms of action, and antidepressant activities. Profound differences between receptor affinity and transporter affinity, pharmacokinetics, regioselectivity in the formation of metabolites, and toxicity are observed for mianserin and mirtazapine and their antidepressant mechanisms of action. The pyridine ring increases the polarity of the molecule and decreases the measured partition coefficient and the basicity. Mianserin is a potent inhibitor of NET , whereas mirtazapine has negligible effects on the inhibition of NET (pKi = 7.1 vs. 5.8 respectively).

Mirtazapine Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Mirtazapine Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 281)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Zibo Hangyu Biotechnology Development Co., Ltd
+86-0533-2185556 +8617865335152
Mandy@hangyubiotech.com China 10986 58
Shaanxi TNJONE Pharmaceutical Co., Ltd
+8618092446649
sarah@tnjone.com China 1143 58
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29791 60
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21634 55
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28172 58
Xiamen AmoyChem Co., Ltd
+86-86-5926051114 +8618959220845
sales@amoychem.com China 6383 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873
sales@chemdad.com China 39894 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49374 58
SIMAGCHEM CORP
+86-13806087780
sale@simagchem.com China 17365 58

61337-67-5()Verwandte Suche:


  • 1,2,3,4,10,14B-HEXAHYDRO-2-METHYLPYRAZINO[2,1-A]PYRIDO[2,3-C][2]BENZAZEPINE
  • 1,2,3,4,10,14b-Hexahydro-2-methylpyrazino[2,1-α]pyrido[2,3-c][2]benzazepine
  • Mirtazepine, 1,2,3,4,10,14b-Hexahydro-2-methylpyrazino[2,1-a]pyrido[2,3-c][2]benzazepine
  • ORG-3770
  • MIRTAZANINE
  • MIRTAZEPINE
  • REMERON
  • 1,2,3,4,10,14b-Hexahydro-2-methylpyrazino[2,1-a]pyrido[2,3-c]benzazepine
  • 1-a)pyrido(2,3-c)(2)benzazepine,1,2,3,4,10,14b-hexahydro-2-methyl-pyrazino(
  • 2-Methyl-1,2,3,4,10,14b-hexahydropyrazino[2,1-a]pyrido[2,3-c][2]benzazepine
  • 6-Azamianserin
  • Mepirzepine
  • Pyrazino[2,1-a]pyrido[2,3-c][2]benzazepine, 1,2,3,4,10,14b-hexahydro-2-methyl-
  • ZISPIN
  • Mitazapine
  • Mirtazapine
  • Remergon
  • Org3770 / 6-Azamianserin
  • Mirtazapine solution
  • 2-methyl-1,2,3,4,10,14b-hexahydrobenzo[c]pyrazino[1,2-a]pyrido[3,2-f]azepine
  • Mitrazapine Hemihydrate
  • Mirtazapine (350 mg)
  • Mirtazapine (350 mg)F0D1550.999mg/mg(an)
  • Mirtazapine API
  • (7S)-5-Methyl-2,5,19-triazatetracyclo[13.4.0.0^{2,7}.0^{8,13}]nonadeca-1(19),8,10,12,15,17-hexaene
  • Mirtazapine Remeron
  • Mirtazne
  • Mirtazapine for system suitability (Y0000721)
  • Mirtazapine Hemihydrate USPQ: What is Mirtazapine Hemihydrate USP Q: What is the CAS Number of Mirtazapine Hemihydrate USP Q: What is the storage condition of Mirtazapine Hemihydrate USP
  • Mirtazapine (Y0000705)Q: What is Mirtazapine (Y0000705) Q: What is the CAS Number of Mirtazapine (Y0000705)
  • 61337-67-5
  • C17H19N3
  • C17H19N312
  • Pharmaceutical raw material
  • Serotonin
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
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