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KMID : 0043319960190060480
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Archives of Pharmacal Research
1996 Volume.19 No. 6 p.480 ~ p.485
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Inhibitory actions of the antidepressant/antipanic drug phenelzine on brain GABA transaminase
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Yoo Byung-Kwon
Hong Joung-Woo
Suk Jae-Wook
Ahn Jee-Yin
Yoo Jeong-Suk
Lee Kil-Soo
Cho Sung-Woo
Choi Soo-Young
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Abstract
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Brain GABA transaminase is inactivated by preincubation with antidepressant/antipanic drug pheneizine (ethylphenylhydrazine) (mixing molar ratio 10:1) at pH 7.4. The reaction of enzyme with phenelzine was monitored by absorption and fluorescence spectroscopic methods. The inactive enzyme was fully reconstituted by addition of cofactor pyridoxal-5-phosphate. This result implies that the blocking of 1 mol of pyridoxal-5-phosphate per enzyme dimer is needed for inactivation of the enzyme. The time course of the reaction is significantly affected by the substrate .alpha.-ketoglutarate, which afforded complete protection against the loss of catalytic activity. The kinetic studies shows that phenelzine reacts with the cofactor of enzyme with a second-order rate constant of . It is postulated that the antidepressant/antipanic drug phenelzine is able to elevate the neurotransmitter GABA levels in central nervous system by inhibitory action on GABA degradative enzyme GABA transaminase.
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KEYWORD
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Brain GABA transminase, Antidepressant/antipanic drug, Phenelzine
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