Propranolol is a non-selective β-adrenergic receptor (βAR) antagonist, which has high affinity for β1AR and β2AR with Ki value of 1.8 nM and 0.8 nM, respectively. Propranolol inhibited the binding of [3H]-DHA to rat meninges with an IC50 of 12 nM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 60 mg/mL|
|Related Adrenergic Receptor Products|
(S)-(-)-Propranolol hydrochloride, the active enantiomer of propranolol, is a β-Adrenoceptor (β-Adrenergic Receptor) antagonist with log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively.
Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension.
Guanabenz (GBZ, GA, Wytensin, Wy-8678) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.
Fluticasone furoate is an inhaled corticosteroid/long-acting beta-agonist combination with a prolonged bronchodilator duration of action. It is used for the treatment of non-allergic and allergic rhinitis administered by a nasal spray.
Midodrine belongs to the class of medications known as vasopressors. It is an adrenergic alpha-1 agonist.
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