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| | PYRILAMINE MALEATE Basic information |
| | PYRILAMINE MALEATE Chemical Properties |
| Melting point | 101-103°C | | storage temp. | 2-8°C | | solubility | Very soluble in water, freely soluble in ethanol (96 per cent). | | form | neat | | color | White | | Water Solubility | Soluble in water at 100mg/ml | | λmax | 310nm(EtOH)(lit.) | | Merck | 14,7984 | | Stability: | Stability Combustible. Incompatible with strong oxidizing agents. | | LogP | 2.751 (est) | | CAS DataBase Reference | 59-33-6(CAS DataBase Reference) | | EPA Substance Registry System | Pyrilamine maleate (59-33-6) |
| Hazard Codes | Xn | | Risk Statements | 22-36/37/38 | | Safety Statements | 26-36/37 | | WGK Germany | 3 | | RTECS | UT1225000 | | TSCA | Yes | | HS Code | 2933399090 | | Toxicity | LD50 orally in mice: 338 mg/kg (Hunziker) |
| | PYRILAMINE MALEATE Usage And Synthesis |
| Description | 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 Gq/11 protein-coupled form of the receptor and to promote a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/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. | | Chemical Properties | solid | | Uses | 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. | | Uses | A histamine H1 receptor antagonist | | Uses | Mepyramine maleate is used as bulk pharmaceutical (antihistaminic). Product Data Sheet | | Brand name | Histavet-P [Veterinary] (Schering-Plough Animal Health); Pymafed (HoechstRoussel). | | General Description | 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. | | General Description | White crystals or powder. Melting point 100-101°C. Bitter saline taste. An antihistaminic medicine. | | Air & Water Reactions | Water soluble. | | Reactivity Profile | 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. | | Fire Hazard | Flash point data for PYRILAMINE MALEATE are not available, however PYRILAMINE MALEATE is probably combustible. | | Biological Activity | 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. | | Safety Profile | 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. | | storage | Room temperature |
| | PYRILAMINE MALEATE Preparation Products And Raw materials |
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