{"refrec":{"BRefID":262017,"RR":"<b>Czerwiec, E.; De Backer, J.-P.; de Potter, W.; Vauquelin, G.</b> (1993). Selective masking of M1-receptors in calf retina membranes by the venom of the marine snail <i>Conus tessulatus</i>. <i>Neurochemistry International 23(1)</i>: 79-85. <a href=\"https://dx.doi.org/10.1016/0197-0186(93)90146-V\" target=\"_blank\">https://dx.doi.org/10.1016/0197-0186(93)90146-V</a>","BEntID":254036,"PublicFlag":1,"CheckedFlag":1,"wosflag":1,"vabbflag":1,"RefStringPartII":". <i>Neurochemistry International 23(1)</i>: 79-85. <a href=\"https://dx.doi.org/10.1016/0197-0186(93)90146-V\" target=\"_blank\">https://dx.doi.org/10.1016/0197-0186(93)90146-V</a>","DocTypID":8,"DocType":"Journal article","MarineFlag":1,"FreshFlag":0,"BrackishFlag":0,"TerrestrialFlag":0,"Authorstring":"Czerwiec, E.; De Backer, J.-P.; de Potter, W.; Vauquelin, G.","OrigTitleTranslFlag":0,"Authorstringtrunc":"Czerwiec, E. <i>et al.</i>","Englishabstract":"The non discriminatory antagonist [<sup>3</sup>H]QNB labels M1- and M2-muscarinic receptors in calf retina membranes. Crude venom from the marine gastropod <i>Conus tessulatus</i> produces a partial decrease in [<sup>3</sup>H]QNB binding. The total number of sites (560 ± 13 fmol/mg protein in control experiments) decreases to 370 ± 10 fmol/mg protein whereas the affinity of the radioligand is unaffected (<i>K</i><sub>D</sub> = 0.42 ± 0.01 nM and 0.46 ± 0.02 nM, respectively). This process is venom concentration-dependent, quasi-irreversible, and calcium-dependent. Proteolytic activity can not be detected.The partial effect of the venom is related to preferential masking of the M1-receptors. Competition curves of the M1-selective antagonist pirenzepine are shallow in control experiments: 45% of the receptors are of the M1-type (<i>K</i><sub>i</sub> = 45 ± 6 nM) while the remaining are of the M2-type (<i>K</i><sub>i</sub> = 1.0 ± 0.2 μM). In venom-treated membranes, only a low affinity site (M2-receptors, <i>K</i><sub>i</sub> = 1.5 ± 0.4 μM) is detected by pirenzepine competition binding. Saturation binding experiments reveal that the venom causes a substantial decrease in the number of high affinity sites for [<sup>3</sup>H]pirenzepine without affecting its <i>K</i><sub>D</sub> (23 ± 4 nM and 20 ± 6 nM in control- and venom-treated membranes respectively). The venom produces a leftward shift of the carbachol/[<sup>3</sup>H]QNB competition binding curve, but the ability of 0.1 mM GTP to confer a rightward shift of the competition curve is not affected. These data suggest that the venom from <i>Conus tessulatus</i> contains one or more components which specifically shield part of the M1-receptors (75% in calf retina membranes), leaving the M2-receptors and their functional coupling to G proteins unaffected.","AbstractOtherLang":null,"BibLvlCode":"AS","StandardTitle":"Selective masking of M1-receptors in calf retina membranes by the venom of the marine snail <i>Conus tessulatus</i>","OrigTitleLangCode":"en","OrigTitleLangCodeExtended":"eng","OrigTitleLangID":15,"DateLastModified":{"date":"2024-12-10 01:33:17.368041","timezone_type":1,"timezone":"+01:00"},"UserAccessRight":null,"UserAccID":null,"AuthorKeywords":null,"OtherDescriptors":null,"Notes":null,"AnaPub":1993,"MonPub":null,"DateUpdate":"2022-05-10","DateCreate":"2016-10-03","SecASFANote":null,"ConfID":null,"PeerRev":1,"VlizCoreFlag":1,"WoScode":"WOS:A1993LK65400008","VABBcode":null,"OpenAcc":0,"DOI":"10.1016/0197-0186(93)90146-V"},"refs":null,"anarec":{"AnaID":262017,"PubliDate":1993,"Pagination":"79-85","XtraPublOfAnaID":null,"ISBN":null,"Volume":"23","Issue":"1","BRefMon":null,"BRefMonRR":null,"BRefXtra":null,"BRefXtraRR":null,"SerBRefID":275301,"SerRR":"Neurochemistry International. 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