Selective antagonists for GABA.sub.rho receptor
AssigneeThe Regents of the University of California
InventorsRicardo Miledi, Larry E. Overman, Yoshinori Murata, Richard M. Woodward
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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.
Claims9
A compound having the formula:
- ##STR7## wherein each of R.sup.2, R.sup.3, R.sup.4, and R.sup.5 is hydrogen;
- and R.sup.6 is selected from the group consisting of C.sub.6-10 aryl, branched or straight chain C.sub.-10 alkyl, and branched or straight chain C.sub.1-10 alkoxy;
- or a pharmaceutically acceptable salt thereof.
A composition comprising:
- a pharmaceutically acceptable carrier;
- and
- a pharmaceutically effective amount of a compound having the formula:
- ##STR8## wherein each of R.sup.2, R.sup.3, R.sup.4, and R.sup.5 is hydrogen;
- and R.sup.6 is selected from the group consisting of C.sub.1-10 aryl, branched or straight chain C.sub.1 -10 alkyl, and branched or straight chain C.sub.1-10 alkoxy;
- and pharmaceutically acceptable salts thereof.
A method for modulating the responsiveness of mammalian GABA.sub.rho receptors comprising exposing mammalian GABA.sub.rho receptors to an effective receptor-modulating amount of a compound having the formula:
- ##STR9## wherein each of R.sup.2, R.sup.3, R.sup.4, and R.sup.5 is hydrogen;
- and R.sup.6 is selected from the group consisting of C.sub.6-10 aryl, branched or straight chain C.sub.1-10 alkyl, and branched or straight chain C.sub.1-10 alkoxy;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.