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Presynaptic block of transmission in the insect CNS by mono- and di-galactosyl analogues of vespulakinin 1, a wasp (Paravespula maculifrons) venom neurotoxin


Presynaptic block of transmission in the insect CNS by mono- and di-galactosyl analogues of vespulakinin 1, a wasp (Paravespula maculifrons) venom neurotoxin



Comparative Biochemistry and Physiology. C Comparative Pharmacology and Toxicology 105(2): 189-196



ISSN/ISBN: 0742-8413

PMID: 8103727

DOI: 10.1016/0742-8413(93)90193-o

1. The pharmacological properties of four synthetic analogues of the wasp neurotoxin, Vespulakinin 1, were studied using a cascade of mammalian smooth muscle preparations and the synaptic transmission from the cockroach cercal nerves to a giant interneuron. 2. All analogues have an extremely slow bradykinin-like effect on the smooth muscles. The carbohydrate-free and the two mono-glycosylated analogues are about equally active with bradykinin. 3. The double glycosylated derivative is about 5 times more potent than bradykinin. 4. All analogues have two different effects on synaptic transmission in the insect CNS--at first a direct and reversible block of excitatory nicotinic transmission with a concurrent activation of the inhibitory GABA-ergic system and, secondly, a delayed irreversible block of the transmission, comparable to the block described earlier for bradykinin and Thr6-bradykinin. 5. For the synaptic transmission in the insect CNS the double glycosylated kinin is about 5 times more potent than bradykinin.

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Accession: 002676799

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