[3H]GBR 12935 binding in platelets: A possible association with cytochrome P-450IID6?

Add time:09/10/2019    Source:sciencedirect.com

The nature of [3H] {1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl) piperazine dihydrochloride} (GBR 12935) binding to human platelets was investigated. A common property of the inhibitors of this binding was their association with the cytochrome P-450 system. cis-Flupenthixol and {1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-[3-phenylpropyl]piperazine dihydrochloride} (GBR 12909) biphasically inhibited the binding. The fraction of [3H]GBR 12935 binding that was inhibited by low concentrations of cis-flupenthixol was sensitive to protease treatment. [3H]GBR 12935 binding to this fraction was saturable and of high affinity (Kd 4.5 nM). The present results reveal that [3H]GBR 12935 binds to multiple sites in platelets and suggest that part of the binding is associated with cytochrome P-450IID6.

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