Name | Pyrilamine Maleate |
Synonyms | paramal pymafed paraminylmaleate Pyrilamine Maleate MEPYRAMINE MALEATE neo-anterganmeleate MEPYRAMINE MALEATE SALT n-dimethylaminoethyl-n-p-methoxy-alpha-aminopyridinemaleate n-p-methoxybenzyl-n'-n'-dimethyl-n-alpha-pyridylethylenediaminemaleate |
CAS | 59-33-6 |
EINECS | 200-422-7 |
Molecular Formula | C21H27N3O5 |
Molar Mass | 401.46 |
Melting Point | 101-103°C |
Water Solubility | Soluble in water at 100mg/ml |
Solubility | Very soluble in water, freely soluble in ethanol (96 per cent). |
Appearance | neat |
Color | White |
Maximum wavelength(λmax) | ['310nm(EtOH)(lit.)'] |
Merck | 14,7984 |
Storage Condition | 2-8°C |
Stability | Stability Combustible. Incompatible with strong oxidizing agents. |
In vitro study | Mepyramine maleate is an antagonist of histamine H1 receptor, with K d s of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pK d of 9.4 for H1 receptor. Mepyramine binds to the H1 receptor with different K d s in Guinea pig brain (0.8 nM), rat brain (9.1 nM) and DDT1-MF-2 and BC3H1 cell (276 nM). Mepyramine decreases the InsP levels in CHO-gpH1 cells, with log EC 50 of -7.94 ± 0.11, and reduces the the maximal response to ATP in CHO-gpH1 cells. |
In vivo study | Mepyramine obviously decreases the second phase of nociceptive response via i.p at 10 and 20 mg/kg, but shows no significant effect at 5 mg/kg in rats. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R22 - Harmful if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
WGK Germany | 3 |
RTECS | UT1225000 |
TSCA | Yes |
HS Code | 2933399090 |
Toxicity | LD50 orally in mice: 338 mg/kg (Hunziker) |
EPA chemical substance information | information provided by: ofmpeb.epa.gov (external link) |
biological activity | Mepyramine maleate is a first generation antihistamine that is a histamine H1 receptor antagonist, the Kd values for the H2 and H3 receptors were 0.8 nM,5200 nM and> 3000 nM, respectively, and the pKd value for the H1 receptor was 9.4. |
Target | Kd: 0.8 nM (Histamine H1 receptor), 5200 nM (Histamine H2 receptor), >3000 nM (Histamine H3 receptor) pKd: 9.4 (Histamine H1 receptor) |