Abstract:
:Gabaculine, a conformationally restricted analogue of GABA, is (i) a moderately potent inhibitor (IC(50) 69 muM) of the sodium-dependent uptake of GABA in rat brain slices, (ii) ineffective at 100 muM as an inhibitor of the sodium-independent binding of GABA to membranes from rat brain, (iii) a relatively weak inhibitor (IC(50) > 1 mM) of glutamate decarboxylase activity in tracts of rat brain, and (iv) a very potent inhibitor (IC(50) 3 muM) of the transamination of GABA catalyzed by extracts of rat brain mitochondria. Inhibition of transamination is time-dependent and follows pseudo-first order kinetics, which is consistent with gabaculine acting as a catalytic inhibitor at the active site.
journal_name
Neurosci Lettjournal_title
Neuroscience lettersauthors
Allan RD,Johnston GA,Twitchin Bdoi
10.1016/0304-3940(77)90124-0subject
Has Abstractpub_date
1977-01-01 00:00:00pages
51-4issue
1eissn
0304-3940issn
1872-7972pii
0304-3940(77)90124-0journal_volume
4pub_type
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