LY134046

LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT) with cardiovascular activity. LY134046 causes sustained reductions in mean arterial blood pressure and heart rate, but no significant reductions in norepinephrine concentrations in the rat brain. LY134046 does not interact with adrenergic or cholinergic receptors, and its hypotensive and bradycardic effects do not require neurogenic tension. LY134046 (40 mg/kg/day) causes sustained and significant inhibition of hypothalamic and brainstem NMT activity, resulting in central norepinephrine depletion.