T. Piek , B. Hue , H. Le Corronc , P. Mantel , M. Gobbo , R. Rocchi
{"title":"黄蜂毒液神经毒素vespulakinin 1的单半乳糖和双半乳糖类似物在昆虫中枢神经系统中的突触前传导阻滞","authors":"T. Piek , B. Hue , H. Le Corronc , P. Mantel , M. Gobbo , R. Rocchi","doi":"10.1016/0742-8413(93)90193-O","DOIUrl":null,"url":null,"abstract":"<div><p>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 cereal nerves to a giant interneuron.</p><p>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.</p><p>3. The double glycosylated derivative is about 5 times more potent than bradykinin.</p><p>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 Thr<sup>6</sup>-bradykinin.</p><p>5. For the synaptic transmission in the insect CNS the double glycosylated kinin is about 5 times more potent than bradykinin.</p></div>","PeriodicalId":72650,"journal":{"name":"Comparative biochemistry and physiology. C: Comparative pharmacology","volume":"105 2","pages":"Pages 189-196"},"PeriodicalIF":0.0000,"publicationDate":"1993-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0742-8413(93)90193-O","citationCount":"15","resultStr":"{\"title\":\"Presynaptic block of transmission in the insect CNS by mono- and di-galactosyl analogues of vespulakinin 1, a wasp (Paravespula maculifrons) venom neurotoxin\",\"authors\":\"T. Piek , B. Hue , H. Le Corronc , P. Mantel , M. Gobbo , R. Rocchi\",\"doi\":\"10.1016/0742-8413(93)90193-O\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>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 cereal nerves to a giant interneuron.</p><p>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.</p><p>3. The double glycosylated derivative is about 5 times more potent than bradykinin.</p><p>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 Thr<sup>6</sup>-bradykinin.</p><p>5. For the synaptic transmission in the insect CNS the double glycosylated kinin is about 5 times more potent than bradykinin.</p></div>\",\"PeriodicalId\":72650,\"journal\":{\"name\":\"Comparative biochemistry and physiology. C: Comparative pharmacology\",\"volume\":\"105 2\",\"pages\":\"Pages 189-196\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1993-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/0742-8413(93)90193-O\",\"citationCount\":\"15\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Comparative biochemistry and physiology. C: Comparative pharmacology\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/074284139390193O\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Comparative biochemistry and physiology. C: Comparative pharmacology","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/074284139390193O","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Presynaptic block of transmission in the insect CNS by mono- and di-galactosyl analogues of vespulakinin 1, a wasp (Paravespula maculifrons) venom neurotoxin
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 cereal 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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