title: Kinetics of choline uptake into isolated rat forebrain microvessels: evidence of endocrine modulation.
abstract: The active uptake of [methyl-3H]choline into isolated rat brain microvessel suspension was studied as a likely guide to the transport of choline across the blood-brain barrier. The method consisted primarily of incubation of the suspension with a fixed concentration of labeled choline in the presence of increasing concentrations of unlabeled choline or any other inhibitor (I) of active uptake, defined as the difference in uptake at 37 degrees and 0 degrees C. From the linear regression of (1/V) against [I], the following values of Vmax (nmol g-1 min-1) and Km (microM) were obtained for choline: 2-month-old males, 10.6 +/- 3.8 and 6.1 +/- 0.9; 3-month old random females, 28.4 +/- 5.9 and 12.6 +/- 4.0; females at metaestrus, 17.8 +/- 10.3 and 8.3 +/- 5.0; at diestrus, 31.1 +/- 9.3 and 13.0 +/- 2.6; at proestrus, 54.9 +/- 2.2 and 14.0 +/- 1.5; at estrus, 19.2 +/- 2.2 and 2.6 +/- 1.7. The differences between males and random females (p less than 0.018) and between females at proestrus and estrus (p less than 0.005) are significant. It is suggested that these inter- and intrasex variations in choline uptake reflect a dynamic adjustment of supply in accordance with brain demand for choline at the time of assay. Hemicholinium-3 was an effective inhibitor of choline uptake, Ki = 14.0 +/- 8.5 microM; dimethylaminoethanol was much less effective; and imipramine had no measurable effect.
authors: Department of Physiology and Pharmacology, Tel Aviv University, Israel.
authors: M
authors: M
authors: Shimon
authors: Y
authors: Y
authors: Egozi
authors: Y
authors: Y
authors: Kloog
authors: M
authors: M
authors: Sokolovsky
authors: S
authors: S
authors: Cohen
mesh_terms: D000818:Animals; D001693:Biological Transport, Active / Q000187:drug effects; D001812:Blood-Brain Barrier; D002794:Choline / Q000378:metabolism*; D003642:Deanol / Q000494:pharmacology; D004027:Diencephalon / Q000098:blood supply*; D004971:Estrus / Q000378:metabolism; D005260:Female; D006426:Hemicholinium 3 / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D008833:Microcirculation / Q000378:metabolism; D051381:Rats; D013687:Telencephalon / Q000098:blood supply*
chemical_list: D003642:Deanol; D006426:Hemicholinium 3; D002794:Choline