A highly lipophilic agent that blocks both β1 and β2 adrenergic receptors with equal potency. Has no effect on α-adrenergic receptors. Also binds to 5HT-1B receptors with high affinity (Ki = 17 nM) in contrast to 5HT-1D receptors (Ki = 10.2 µM). Readily enters the central nervous system. Blocks phospholipase D-derived diacylglycerol (DAG) formation by inhibiting phosphatidate phosphohydrolase. Useful tool for discriminating between phospholipase D- or phospholipase C-mediated DAG production. An anti-hypertensive agent that is also used in the treatment of cardiac arrhythmias.
β1 and β2 adrenergic receptors
Product does not compete with ATP.
Target Ki: 17 nM for 5HT-1B receptors
Cell permeable: no
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