Syntheses of Novel Piperidin-4-ylphosphinic Acid, and Piperidin-4-ylphosphonic Acid Analogues of the Inhibitory Neurotransmitter 4-Aminobutyric Acid (GABA). -The novel acids (V)-(VIII) are synthesized utilizing a sequential Pudovik addition followed by a modified Barton deoxygenation and acidic hydr
The preparation of tritiated E- and Z-4-aminobut-2-enoic acids, conformationally restricted analogues of the inhibitory neurotransmitter 4-aminobutanoic acid (GABA)
✍ Scribed by Rujee K. Duke; Robin D. Allan; Colleen A. Drew; Graham A. R. Johnston; Kenneth N. Mewett; Mervyn A. Long; Chit Than
- Book ID
- 102901479
- Publisher
- John Wiley and Sons
- Year
- 1993
- Tongue
- French
- Weight
- 626 KB
- Volume
- 33
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
A synthesis of [^3^H]E‐ and [^3^H]Z‐4‐aminobut‐2‐enoic acids from methyl 4‐N‐phthalimidobut‐2‐ynoate by catalytic hydrogenation using tritium gas in the presence of a homogeneous catalyst, tris(triphenylphosphine)rhodium(I) chloride, is reported. HPLC separation of the E‐ and Z‐isomers, and the saturated analogue, 4‐aminobutanoic acid (GABA), is also described.
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The effects of the GABA analogues, cis-and trans-4aminocrotonic acid (ACA) on GABA A receptor function and GABA uptake, together with the presence of -1 subunit mRNA and putative GABA C receptors, were studied in primary cultures of neocortical neurons and cerebellar granule cells. Both isomers indu