TRIMIPRAMINE MALEATE SALT Struktur

Trimipraminhydrogenmaleat

Bezeichnung:Trimipraminhydrogenmaleat

CAS-Nr521-78-8

Englisch Name:TRIMIPRAMINE MALEATE SALT

CBNumberCB3104538

SummenformelC24H30N2O4

Molgewicht410.51

MOL-Datei521-78-8.mol

Synonyma

Trimipraminhydrogenmaleat

Trimipraminhydrogenmaleat physikalisch-chemischer Eigenschaften

Schmelzpunkt	141-143°C
Flammpunkt	11 °C
storage temp.	2-8°C
Löslichkeit	chloroform: soluble50 mg/ml, clear, colorless to faintly yellow
Aggregatzustand	powder
Farbe	white
EPA chemische Informationen	Trimipramine maleate (521-78-8)

Sicherheit

Kennzeichnung gefährlicher	Xn,T,F
R-Sätze:	22-36/37/38-63-36/38-23/25-39/23/24/25-23/24/25-11
S-Sätze:	26-36-45-33-24-16-7-36/37
RIDADR	3249
WGK Germany	3
RTECS-Nr.	HN9260000
HazardClass	6.1(b)
PackingGroup	III
HS Code	2933996100

Gefahreninformationscode (GHS)

TRIMIPRAMINE MALEATE SALT Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
R63:Kann das Kind im Mutterleib möglicherweise schädigen.
R36/38:Reizt die Augen und die Haut.
R23/25:Giftig beim Einatmen und Verschlucken.
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.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
S33:Maßnahmen gegen elektrostatische Aufladungen treffen.
S24:Berührung mit der Haut vermeiden.
S16:Von Zündquellen fernhalten - Nicht rauchen.
S7:Behälter dicht geschlossen halten.
Chemische Eigenschaften
White Crystalline Solid
Originator
Surmontil Wyeth-Ayerst,Laboratories
Verwenden
Antidepressant; serotonin transport blocker that also blocks norepinephrine uptake.
Verwenden
Antidepressant;Noradrenaline uptake inhibitor
Manufacturing Process
Bis(3-dimethylamino-2-methylpropyl)-5-iminodibenzylyl carboxylic acid at 185-250°C up to discontinue a separation of oxyde carbonique. The product was dissolved in ether, then washed with the hydrochloric acid. Then this solution was extracted with ether. The solvent was evaporated under vacuum, to give pure oil bis(3-dimethylamino-2-methyl-1-propyl)-5-iminodibenzyle with boiling point 153-154°C at 0.4 mm. Maleate of bis(3-dimethylamino-2-methyl- 1-propyl)-5-iminodibenzyle have melting point 145-146°C.
Trademarks
Surmontil (Odyssey).
Therapeutic Function
Antidepressant
Allgemeine Beschreibung
For details of chemical nomenclature, consult the descriptionof imipramine. Replacement of hydrogen with an -methylsubstituent produces a chiral carbon, and trimipramine(Surmontil) is used as the racemic mixture. Biological propertiesreportedly resemble those of imipramine.
Biologische Aktivität
trimipramine (maleate) is a potent antagonist of histamine h1 receptor, serotonin 5-ht2a, and α1-adrenergic receptors [1].the histamine h1 receptor is widely expressed tissues, such as smooth muscles, vascular endothelial cells, heart, and the central nervous system. histamine h1 receptor (h1r) antagonists are very effective drugs alleviating the symptoms of allergic reactions [2]. 5-ht2a receptor shows constitutive activity. variations in5-ht2a receptor can produce profound alterations in cognitive states [3]. the adrenergic receptors play an important role in modulating sympathetic nervous system activity as well as a site of action for many therapeutic agents. the α1-adrenergic receptor is the prime mediators of smooth muscle contraction and hypertrophic growth. the α1-adrenergic receptor plays an essential role in smooth muscle, growth, neurological, and cardiovascular function [4].trimipramine (maleate) is a tricyclic antidepressant compound that antagonizes several types of neurotransmitter receptors. trimipramine potently antagonized the activity of histamine h1 serotonin 5-ht2a, and α1-adrenergic receptors with the kd value of 0.27 nm, 24 nm, and 24 nm, respectively. trimipramine moderately antagonized the activity of dopamine d2 with the kd of 180 nm. trimipramine inhibited the activity of muscarinic acetylcholine with the kd of 58 nm. trimipramine weakly inhibited the activity of 5-ht2c, d1, α2-adrenergic receptors (kd = 680 nm) [1]. trimipramine (maleate) was a weak to moderate reuptake inhibitor of serotonin (ki = 149 nm for sert), and an extremely weak inhibitor of norepinephrine (ki = 2.5 μm for net) and dopamine (ki = 3.8 μm for dat) reuptake in slices of rat cerebral cortex [5,6].
Biochem/physiol Actions
Antidepressant; serotonin transport blocker that also blocks norepinephrine uptake.
Einzelnachweise
[1] richelson e, nelson a. antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro[j]. journal of pharmacology and experimental therapeutics, 1984, 230(1): 94-102.
[2] shimamura t, shiroishi m, weyand s, et al. structure of the human histamine h1 receptor complex with doxepin[j]. nature, 2011, 475(7354): 65-70.
[3] harvey j a. role of the serotonin 5-ht2a receptor in learning[j]. learning & memory, 2003, 10(5): 355-362.
[4] piascik m t, perez d m. α1-adrenergic receptors: new insights and directions[j]. journal of pharmacology and experimental therapeutics, 2001, 298(2): 403-410.
[5] gross g, xie x, gastpar m. trimipramine: pharmacological reevaluation and comparison with clozapine[j]. neuropharmacology, 1991, 30(11): 1159-1166.
[6] tatsumi m, groshan k, blakely r d, et al. pharmacological profile of antidepressants and related compounds at human monoamine transporters[j]. european journal of pharmacology, 1997, 340(2): 249-258.

Trimipraminhydrogenmaleat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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