4, 5, 6, 7-Tetrahydroisothiazolo [5, 4-c] pyridin-3-ol and related analogs of THIP. Synthesis and biological activity

P Krogsgaard-Larsen, H Mikkelsen…

Index: Krogsgaard-Larsen; Mikkelsen; Jacobsen; Falch; Curtis; Peet; Leah Journal of Medicinal Chemistry, 1983 , vol. 26, # 6 p. 895 - 900

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Citation Number: 50

Abstract

The thio analogues of the GABA (y-aminobutyric acid) agonist THIP (4, 5, 6, 7- tetrahydroisoxazolo [5, 4-c] pyridin-3-01), the GABA uptake inhibitor THPO (4, 5, 6, 7- tetrahydroisoxazolo [4, 5-c] pyridin-3-01), and the glycine antagonist THAZ (5, 6, 7, 8- tetrahydro-4H-isoxazolo [4, 5-d] azepin-3-ol) have been synthesized and tested biologically on single neurons in the cat spinal cord and in vitro by using synaptic membrane ...