N-((4-Methoxyphenyl)methyl)-N',N'-dimethyl-N-2-pyridinyl-1,2-ethan-diamin, (Z)-2-butendioat (1:1)

Bezeichnung:N-((4-Methoxyphenyl)methyl)-N',N'-dimethyl-N-2-pyridinyl-1,2-ethan-diamin, (Z)-2-butendioat (1:1)

CAS-Nr59-33-6

Englisch Name:PYRILAMINE MALEATE

CBNumberCB3677373

SummenformelC21H27N3O5

Molgewicht401.46

MOL-Datei59-33-6.mol

Synonyma

Mepyraminmaleat

N-((4-Methoxyphenyl)methyl)-N',N'-dimethyl-N-2-pyridinyl-1,2-ethan-diamin, (Z)-2-butendioat (1:1)

N-((4-Methoxyphenyl)methyl)-N',N'-dimethyl-N-2-pyridinyl-1,2-ethan-diamin, (Z)-2-butendioat (1:1) physikalisch-chemischer Eigenschaften

Schmelzpunkt	101-103°C
storage temp.	2-8°C
Löslichkeit	Very soluble in water, freely soluble in ethanol (96 per cent).
Aggregatzustand	Solid
Farbe	White
Wasserlöslichkeit	Soluble in water at 100mg/ml
maximale Wellenlänge (λmax)	310nm(EtOH)(lit.)
Merck	14,7984
Stabilität	Stability Combustible. Incompatible with strong oxidizing agents.
LogP	2.751 (est)
CAS Datenbank	59-33-6(CAS DataBase Reference)
EPA chemische Informationen	Pyrilamine maleate (59-33-6)

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-36/37/38
S-Sätze:	26-36/37
WGK Germany	3
RTECS-Nr.	UT1225000
TSCA	Yes
HS Code	2933399090
Toxizität	LD50 orally in mice: 338 mg/kg (Hunziker)

Gefahreninformationscode (GHS)

PYRILAMINE 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.
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
Beschreibung
Mepyramine is a first generation antihistamine that acts as an inverse agonist at the histamine H₁ receptor. It is reported to bind with high affinity to a G_q/11 protein-coupled form of the receptor and to promote a G protein-coupled inactive state of the H₁ receptor that interferes with the G_q/11-mediated signaling of the endogenously expressed receptor, as well as to reduce G protein availability for other non-related receptors associated with this signaling pathway. Mepyramine has been shown to inhibit histamine-induced inositol phosphate production with a log EC₅₀ value of -7.94.
Chemische Eigenschaften
solid
Verwenden
Pyrilamine maleate Selective inverse agonist for the H-1 histamine receptor. Pyrilamine Maleate is commonly utilized as a radioligand ([3H]Mepyramine) binding assay for the H1 receptor. And also used to exhibit blocking ability of KCNQ/M channels which is potentially related to an adverse effect seen in excess intake of antihistamines.
Verwenden
A histamine H1 receptor antagonist
Verwenden
Mepyramine maleate is used as bulk pharmaceutical (antihistaminic). Product Data Sheet
Trademarks
Histavet-P [Veterinary] (Schering-Plough Animal Health); Pymafed (HoechstRoussel).
Allgemeine Beschreibung
Pyrilamine, 2-[4-methoxybenzyl[2-dimethylamino)ethyl]-amino]pyridine, is available as theacid maleate salt (1:1), which is a white crystalline powderwith a faint odor and a bitter, saline taste. The salt is solublein water (1:0.4) and freely soluble in alcohol. A 10% solutionhas a pH of approximately 5. At a pH of 7.5 or above,the free base begins to precipitate.
Pyrilamine differs structurally from tripelennamine byhaving a methoxy group in the para position of the benzylradical. It differs from its more toxic and less potent precursorphenbenzamine (Antergan) by having a 2-pyridyl groupon the nitrogen atom in place of a phenyl group.
Clinically, pyrilamine and tripelennamine are consideredamong the less potent antihistaminics. They are highly potent,however, in antagonizing histamine-induced contractionsof guinea pig ileum. Because of the pronounced localanesthetic action, the drug should not be chewed, but takenwith food.
Allgemeine Beschreibung
White crystals or powder. Melting point 100-101°C. Bitter saline taste. An antihistaminic medicine.
Air & Water Reaktionen
Water soluble.
Reaktivität anzeigen
PYRILAMINE MALEATE is an acidic salt of an amine. Usually does not react as either oxidizing agents or reducing agents but such behavior is not impossible. May be incompatible with isocyanates, halogenated organics, peroxides, phenols (acidic), epoxides, anhydrides, and acid halides. Flammable gaseous hydrogen may be generated in combination with strong reducing agents, such as hydrides.
Health Hazard
SYMPTOMS: Symptoms of exposure to PYRILAMINE MALEATE may include drowsiness, potentiation of the sedative effect of barbituates, fatigues, vertigo, incoordination, tremor, muscle weakness, dryness of the mouth and throat, tinnitus, pupillary dilation, blurred vision, urinary retention, impotence, epigastric and intestinal pain, anorexia, nausea, vomiting, diarrhea, excitation, euphoria, insomnia, nervousness, palpitation, tachycardia, hypotension, hypersensitivity reactions, respiratory depression, coma and delirium.
Brandgefahr
Flash point data for PYRILAMINE MALEATE are not available, however PYRILAMINE MALEATE is probably combustible.
Biologische Aktivität
Selective inverse agonist for the H 1 receptor. Inhibits histamine induced inositol phosphate (InsP) production (log EC50 = -7.94) and intracellular calcium mobilization. Sequesters G q/11 protein, reducing its availability for other receptors associated with the same signaling pathway.
Biochem/physiol Actions
Pyrilamine maleate is a H1 histamine receptor antagonist. Pyrilamine maleate induces sleep in vertebrates. In Cassiopea, it induces concentration dependent dormancy.
Sicherheitsprofil
A human poison by ingestion. An experimental poison by ingestion, subcutaneous, intravenous, and intraperitoneal routes. Experimental reproductive effects. Questionable carcinogen with experimental tumorigenic data. Mutation data reported. An antihistamine. When heated to decomposition it emits toxic fumes of NOx.
Veterinary Drugs and Treatments
Antihistamines are used in veterinary medicine to reduce or help prevent histamine mediated adverse effects; predominantly used in horses.
Lager
Room temperature

N-((4-Methoxyphenyl)methyl)-N',N'-dimethyl-N-2-pyridinyl-1,2-ethan-diamin, (Z)-2-butendioat (1:1) Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

59-33-6, PYRILAMINE MALEATE Verwandte Suche:

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