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- W1995142777 abstract "1. We characterized the binding sites of VA-045 [(+)-eburunamenine-14- carboxylic acid (2-nitroxyethyl)ester] in the rat brain. 2. VA-045 showed no affinity for various types of well-known neurotransmitter-related receptors or channels. However, radiolabeled VA-045 ([3H]VA-045) bound to rat brain membranes in a saturable and reversible manner. The Kd and Bmax values of [3H]VA-045 binding were 58.2 nM and 2685 fmol/mg of protein, respectively. 3. The largest specific binding of [3H]VA-045 was observed in the cerebellum, among seven brain regions, and in subcellular synaptosomes. 4. Specific binding of [3H]VA-045 was inhibited by VA-045 (Ki = 0.06 microM), a levorotatory enantiomer of VA-045 (VA-213) and its structural analog, vinpocentine. Moreover, compounds with calmodulin antagonistic activity inhibited the [3H]VA-045 binding. 5. These results suggest that VA-045 binds to specific sites, which may resemble calmodulin, on synaptic membranes in the brain." @default.
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- W1995142777 date "1996-03-01" @default.
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- W1995142777 title "Partial characterization of binding sites of VA-045, a novel apovincaminic acid derivative, in rat brain membranes" @default.
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- W1995142777 doi "https://doi.org/10.1016/0306-3623(95)02020-9" @default.
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