title: [3H]GBR 12935 binding in platelets: a possible association with cytochrome P-450IID6?
abstract: 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 in 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.
authors.affiliation: Department of Geriatric Medicine, Umeä University, Sweden.
authors.forename: M
authors.initials: M
authors.lastname: Norlén
authors.forename: P
authors.initials: P
authors.lastname: Allard
mesh_terms: D014150:Antipsychotic Agents / Q000494:pharmacology; D001792:Blood Platelets / Q000378:metabolism*; D046508:Culture Techniques; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D018492:Dopamine Antagonists / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D005475:Flupenthixol / Q000494:pharmacology; D006801:Humans; D008024:Ligands; D008120:Lobeline / Q000494:pharmacology; D010879:Piperazines / Q000378:metabolism*; D010880:Piperidines / Q000494:pharmacology; D011802:Quinidine / Q000494:pharmacology
chemical_list: D014150:Antipsychotic Agents; D018492:Dopamine Antagonists; D004791:Enzyme Inhibitors; D008024:Ligands; D010879:Piperazines; D010880:Piperidines; D003577:Cytochrome P-450 Enzyme System; C044630:1-(2 (diphenylmethoxy)ethyl)-4-(3-phenylpropyl)piperazine; D008120:Lobeline; D005475:Flupenthixol; D011802:Quinidine; C026710:budipine