Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: Modulators of neurotransmitter release including substituted guanidines, and N"-aminoguanidines, and N,N'N", N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N'"-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: A compound consisting of a base, a ribose and a fucose, in which the base is a purine or a pyrimidine, the ribose has R.sub.1 and R.sub.2 attached respectively to any two of 2'-O, 3'-O and 5'-O, and the fucose has R.sub.3, R.sub.4 and R.sub.5 attached respectively to any three of 1"-O, 2"-O, 3"-O and 4"-O, wherein each R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 is H, acetate, sulfate, phosphate, or a metallic salt of acetate, sulfate or phosphate; and the base is linked to the ribose via a bond between 9-N of the base and 1'-O of the ribose when the base is a purine or via a bond between 1-N of the base and 1'-C of the ribose when the base is a pyrimidine and the ribose is linked to the fucose via a bond between any one of 2'-O, 3'-O and 5'-O of the ribose and 1"-C of the fucose.

Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: A substantially pure compound of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2, independently, is H, CH.sub.3, CF.sub.3, F, Cl, Br, I, OH, OCH.sub.3, OCF.sub.3, SH, SCH.sub.3, NH.sub.2, N.sub.3, NO.sub.2, CN, COOH, CONH.sub.2, CH.sub.2 CONH.sub.2, or SO.sub.2 NH.sub.2 ;R.sub.3 is H, CH.sub.3, COOH, CONH.sub.2, or COOR where R is C.sub.1-4 alkyl;each R.sub.4, independently, is H or C.sub.1-6 alkyl;X is CH.sub.2, CH.sub.2 CH.sub.2, CH.dbd.CH, or CH.sub.2 CH.sub.2 CH.sub.2 ; ##STR2## each Z, independently, is H, CH.sub.3, or Q where Q is a hydrophobic acyl, benzoyl, phenacetyl, benzyloxycarbonyl, alkoxycarbonyl, or N-methyl-dihydropyridine-3-carbonyl linked to N by an amide bond which is cleavable by an endogenous central nervous system enzyme;D is H or ##STR3## where R.sub.5 is H or C.sub.