Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1994-07-20
1997-05-06
Rotman, Alan L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
546 21, C07F 958, A61K 31675
Patent
active
056271697
ABSTRACT:
Novel phosphinic and phosphonic acid derivatives of pyridine, pyrrole and azepine with utility as antagonists of the GABA.sub.rho receptor are disclosed. These compounds have utility as modulators of the excitability of the central nervous system as mediated by their ability to specifically act on closed-channel binding sites of GABA.sub.rho receptors.
REFERENCES:
.sup.3 H-baclofen and .sup.3 H-Gaba bind to bicuculline-insensitive GABA.sub.B sites in rat brain Hill and Bowery, Nature, 290:149-152, Mar. 12, 1981.
Expression of mammalian .gamma.-aminobutyric acid receptors with distinct pharmacology in Xenopus oocytes Polenzani, et al., Proc. Natl. Acad. Sci. USA, 88:4318-4322, 1991.
Effects of Steroids on .gamma.-Aminobutyric Acid Receptors Expressed in Xenopus Oocytes by Poly(A).sup.+ RNA from Mammalian Brain and Retina Woodward, et al., Mol. Pharm. 41:89-103, 1991.
Characterization of Bicuculline/Baclofen-Insensitive .gamma.-Aminobutyric Acid Receptors Expressed in Xenopus Oocytes I. Effects of CI Channel Inhibitors Woodward, et al., Mol. Pharm., 42:165-173, 1992.
Effects of Hexachlorocyclohexanes in .gamma.-Aminobutyric Acid Receptors Expressed in Xenopus Oocytes by RNA from Mammalian Brain and Retina Woodward, et al., Mol. Pharm., 41:1107-1115, 1992.
Miledi Ricardo
Murata Yoshinori
Overman Larry E.
Woodward Richard M.
Rotman Alan L.
The Regents of the University of California
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