A. Fukunaga, H. Hasegawa, C. Ogawa
Feb 1, 1999
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Comparative biochemistry and physiology. Part C, Pharmacology, toxicology & endocrinology
Abstract
3-Aminopropyl(methyl)phosphinic acid (APMP), a potent agonist of mammalian GABAB receptors, caused prostration in houseflies (Musca domestica L.) on injection into their thoraces, with an ED50 value of 0.42 microgram/fly. The 48-h LD50 values of APMP were estimated to be 0.45 and 5.6 micrograms/fly in the presence and absence of piperonyl butoxide, a mixed-function oxidase inhibitor, respectively. Analogues of APMP, bearing a longer or shorter side chain by a CH2 unit, or a phenyl group in the place of the methyl group, were without effects. In perfusion assays with synaptosomes prepared from the thoracic/abdominal nerve cords of cockroaches (Periplaneta americana L.), 1 mM APMP reduced K(+)-evoked acetylcholine release to 10.4% of the control. These findings indicate that the--physiologically important site of action of APMP, which might be implicated in neurotransmitter release, is present in insect neurons.