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Effects of dineopentyl and dipinacoline ethers of glutamic acid on neuromuscular transmission in locust (Locusta migratoria).

The problem of the relationship between structure of dicarboxylic acid derivatives and their capacity to act on glutamate receptors has been extensively studied in various animal species (Piggot et al. 1975; Walker and James 1980; Puil 1981; Mandelshtam 1983). A number of substances with anticonvulsive properties (Meldrum et al. 1983; Colton and Colton 1985) and other preparations with pharmacological potential were derived from these studies (Simon et al. 1984; Hadberg et al. 1986; Baudry and Lynch 1984). L-glutamic acid is the excitatory transmitter of neuromuscular transmission in insects (Usherwood and Machili 1968). The study of the specific aspects of glutamate reception in neuromuscular synapses therefore is of interest from the viewpoint of comparative neuropharmacology as well as for the development of new drugs with effects targeted on the locomotor activity of this animal species. Glutamate acid receptors are classified in three categories according to the agonist type they are capable of reacting with: N-methyl-D-aspartate, kainate and quisqualate (Nistri and Constanti 1979). Insect muscle fibres contain quisqualate type receptors since they are activated by quisqualic acid while being insensitive to N-methyl-D-aspartate, and can be blocked by diethyl ether of glutamic acid (Usherwood 1981). Previous works on neuromuscular synapses of the locust reported that the capacity to block synaptic transmission is directly proportional to both the length and ramification of alkyl radicals of dicarboxylic acid ethers. Symmetric ethers were shown to be more active than the respective /--ethers of glutamic and/or aspartic acid (Aleksandrov and Baranov 1984; Aleksandrov and Speranski 1985). In the present work the effects of symmetric