Abstract

The present study aimed to further elucidate the pharmacological features, wiht respect to sensitivity to L-BHGA agonists,of the receptors sensitive to β-hydroxy-L-glutamic acid (L-BHGA) in five Achatina giant neurones: PON (periodically oscillating neurone), d-RPLN (dorsal-right parietal large neurone), VIN (visceral intermittently firing neurone), RAPN (right anteior pallial neurone) and v-RCDN (ventrral-right cerebral distinct neurone). Of these neurones, d-RPLN and RAPN were depolarized by L-BHGA, while PON, VIN and v-RCDN were inhibited. Threo-β-hydroxy-DL-aspartic acid markedly depolarized d-RPLN and RAPN (effective potency quotient (EPQ) in relation to the more effective L-BHGA isomer: 1 for d-RPLN and 0.3 for RAPN). This compound produced only slight inhibitory effects on PON, VIN and v-RCDN with EPQs calculated to be<0.03, <0.03 and 0.03, respectively. On the other hand, erythro-β-hydroxy-DL-aspartic acid at 10 −3 M was almost ineffective, except on v-RCDN where it elicited some slight inhibitory effects (EPQ: 0.01). L-Aspartic and D-aspartic acid at 10 −3 M, also had almost no effect except for slight effects of D-aspartic acid on d-RPLN (EPQ: 0.1). N-Methyl-L- and N-methyl-D-aspartic acid were slightly effective only on v-RCDN (EPQ: <0.021 and 0.01 respectively). The other compounds, including β-hydroxypyrroglutamic acid (cyclic BHGA) and proline derivatives, were almost ineffective at 10 −3 M; very weak effects were occasionally observed on some neurones. These results have a two-fold meaning: the relative sensitivities of these neurones to the erythro- and threo-L-BHGA stereoisomers do not correspond to the sensitivities of the stereoisomers of β-hydroxy-DL-aspartic acid and the zwitterionic character of the α-amino group, the presence of a β-hydroxyl group and a C4 or C5 carboxyl group are necessary to produced the effects on these neurones.

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