Insecticidal properties of 3-aminopropyl(methyl)phosphinic acid and its effect on K(+)-evoked release of acetylcholine from cockroach synaptosomes.
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.
Fukunaga
A
A
Department of Life Science and Biotechnology, Shimane University, Matsue, Japan.
Hasegawa
H
H
Ogawa
C
C
Matsuno
A
A
Imamura
K
K
Ozoe
Y
Y
D000109:Acetylcholine / Q000378:metabolism*; D000818:Animals; D005260:Female; D018756:GABA Antagonists / Q000494:pharmacology*; D006793:Houseflies; D007306:Insecticides; D008297:Male; D009943:Organophosphorus Compounds / Q000494:pharmacology*; D010526:Periplaneta / Q000378:metabolism*; D011188:Potassium / Q000494:pharmacology*; D013574:Synaptosomes / Q000378:metabolism*; D005680:gamma-Aminobutyric Acid / Q000494:pharmacology
D018756:GABA Antagonists; D007306:Insecticides; D009943:Organophosphorus Compounds; C068457:3-aminopropyl(methyl)phosphinic acid; D005680:gamma-Aminobutyric Acid; D000109:Acetylcholine; D011188:Potassium