General Description
White crystals or powder. Melting point 100-101°C. Bitter saline taste. An antihistaminic medicine.
Reactivity Profile
PYRILAMINE MALEATE(59-33-6) 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.
Air & Water Reactions
Water soluble.
Health Hazard
SYMPTOMS: Symptoms of exposure to this compound 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 this chemical are not available, however PYRILAMINE MALEATE is probably combustible.
Description
Mepyramine is a first generation antihistamine that acts as an inverse agonist at the histamine H
1 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 H
1 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.
1 Mepyramine has been shown to inhibit histamine-induced inositol phosphate production with a log EC
50 value of -7.94.
1
Chemical Properties
solid
Uses
A histamine H1 receptor antagonist
Uses
Mepyramine maleate is used as bulk pharmaceutical (antihistaminic). Product Data Sheet
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.
Brand name
Histavet-P [Veterinary] (Schering-Plough Animal Health); Pymafed (HoechstRoussel).
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.
Veterinary Drugs and Treatments
Antihistamines are used in veterinary medicine to reduce or help
prevent histamine mediated adverse effects; predominantly used in
horses.
storage
4°C, protect from light