Chlorpheniramine, a histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It has also been used in veterinary applications. One of the most widely used of the classical antihistaminics, it generally causes less drowsiness and sedation than promethazine. Chlorpheniramine binds to the histamine H1 receptor. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms brought on by histamine.
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7, MDA-MB 231, and Ehrlich |
| Preparation method | Exposing cells to various concentrations of Chlorpheniramine for 48 hours. Cells are washed, detached, and counted with a Coulter counter to determine cell growth. |
| Concentrations | Dissolved in water, final concentrations ~500 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Male NC/Nga mice, male ICR mice and female BALB/c mice with atopic dermatitis |
| Formulation | Suspended in 1% (v/v) Tween 80 |
| Dosages | 10 mg/kg |
| Administration | Orally |
| Molecular Weight | 390.86 |
| Formula | C16H19ClN2.C4H4O4 |
| CAS Number | 113-92-8 |
| Solubility (25°C) | DMSO 70 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Histamine Receptor Products |
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| Peptide 401
Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT). |
| Granuliberin R
Granuliberin R is a new mast cell degranulating peptide comes from amphibian, can be isolated from the skin of frog Rana rugosa. |
| Dimethindene maleate
Dimethindene maleate is a selective histamine H1 receptor antagonist with antihistamine activity.Dimethindene maleate may be used in studies related to allergic reactions. |
| 4-Methylhistamine
4-Methylhistamine is a potent agonist of histamine 4 receptor (H4R). |
| H4R antagonist 3
H4R antagonist 3 is a histamine-4 receptor antagonist with an EC50 of ＜10 mM. |
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