Proxyphylline is a methylxanthine and derivative of theophylline. Proxyphylline relaxes smooth muscles, particularly bronchial muscles. This xanthine most likely exerts its effect by inhibiting cAMP or cGMP phosphodiesterases, thereby increasing levels of the second messenger cAMP or cGMP intracellularly. Other mode of actions include an adenosine antagonistic effect on the activity of CD4 lymphocytes and mediator release from mast cells thereby decreasing lung sensitivity to allergens and other substances that cause inflammation. Proxyphylline also acts as a CNS stimulant and exerts a positive chronotropic and inotropic effect on the heart.
Molecular Weight | 238.24 |
Formula | C10H14N4O3 |
CAS Number | 603-00-9 |
Form | Solid |
Solubility (25°C) | DMSO |
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.
[3] Paweł Borowiecki, et al. Chemoenzymatic Synthesis of Proxyphylline Enantiomers
Related Adenosine Receptor Products |
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A3AR agonist 1
A3AR agonist 1 is an A3AR agonist (Ki: 25.8 nM). |
A3AR agonist 2
A3AR agonist 2 a selective A3AR agonist (Ki: 22.1 nM). |
Inupadenant hydrochloride
Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. |
A1/A3 AR antagonist 3
A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with high affinity at low-micromolar to low-nanomolar. |
Adenosine receptor antagonist 4
Adenosine receptor antagonist 4 is an adenosine A1 receptor antagonist with a Ki of 101 nM for human A1 receptor. |
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