LY 78335 (DCMB) is a brain-penetrant phenylethanolamine-N-methyltransferase ( PNMT ) inhibitor with a K i of 0.09 μM. LY 78335 acts as an α₂-adrenoceptor inhibitor with an IC50 of 10 μM. LY 78335 increases spontaneous locomotor activity in rats. LY 78335 increases extracellular concentration of 3-methoxy-4-hydroxyphenylglycol (MHPG) in rat hypothalamus. LY 78335 prevents growth hormone (GH) secretion in rats. LY 78335 can be used for the research of depression [1].
In Vivo, LY 78335 (DCMB) (50 mg/kg; i.p.) inhibits α2-adrenoceptor function in the hypothalamus of rats[1].
References:
[1]. Fuller RW, et al. Inhibition of phenylethanolamine N-methyltransferase by benzylamines. 2. In vitro and in vivo studies with 2,3-dichloro-methylbenzylamine. J Med Chem. 1973 Feb;16(2):106-9.
[2]. Kuboia M, et al. Effect of a phenylethanolamine N-methyltransferase inhibitor, 2,3-dichloro-alpha-methylbenzylamine, on the alpha-2-adrenoceptor function in the hypothalamus in rats. Neuropsychobiology. 1996;33(3):132-7.
In Vivo, LY 78335 (DCMB) (50 mg/kg; i.p.) inhibits α2-adrenoceptor function in the hypothalamus of rats[1].
References:
[1]. Fuller RW, et al. Inhibition of phenylethanolamine N-methyltransferase by benzylamines. 2. In vitro and in vivo studies with 2,3-dichloro-methylbenzylamine. J Med Chem. 1973 Feb;16(2):106-9.
[2]. Kuboia M, et al. Effect of a phenylethanolamine N-methyltransferase inhibitor, 2,3-dichloro-alpha-methylbenzylamine, on the alpha-2-adrenoceptor function in the hypothalamus in rats. Neuropsychobiology. 1996;33(3):132-7.