title: Effects of streptozotocin-induced diabetes on neuronal sigma receptors in the rat brain.
abstract: To study the effect of diabetes mellitus on the density of sigma receptors, in vitro binding experiments were conducted in whole brain homogenate membranes of 5-week and 10-week control rats and streptozotocin (STZ)-induced diabetic rats. sigma-1 Receptors were labelled with [3H](+)-pentazocine while sigma-2 receptors were labelled with [3H] 1,3-di-o-tolylguanidine (DTG) in the presence of 0.5 microM (+)-pentazocine to mask sigma-1 sites. Non-specific binding was determined in the presence of 20 microM haloperidol. Scatchard analysis revealed a 27% (p<0.01) decreased in sigma-1 receptor density and a 33% (p<0.01) decreased in sigma-2 receptor density in whole brain of 10-week STZ-diabetic rats. No statistically significant difference was found in the sigma receptor content of 5-week STZ-diabetic rats. These results provide evidence that neuronal sigma receptors are reduced in 10-week STZ-diabetic rats and suggest that changes in sigma receptors may play a role in diabetes related abnormalities. Further evaluation is required to determine whether changes observed in the brain are homogeneous for either or both sigma receptor subtypes as well as potential links between other CNS receptor changes previously observed in STZ-induced diabetic rats.
authors.affiliation: Radiopharmaceutical Division R&D, Australian Nuclear Science and Technology Organisation, NSW.
authors.forename: K
authors.initials: K
authors.lastname: Mardon
authors.forename: M
authors.initials: M
authors.lastname: Kassiou
authors.forename: A
authors.initials: A
authors.lastname: Donald
mesh_terms: D000701:Analgesics, Opioid / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001786:Blood Glucose / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D003921:Diabetes Mellitus, Experimental / Q000378:metabolism*; D006029:Glycosuria / Q000139:chemically induced; D006146:Guanidines / Q000378:metabolism / Q000494:pharmacology; D006220:Haloperidol / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D010423:Pentazocine / Q000378:metabolism / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D017480:Receptors, sigma / Q000145:classification / Q000378:metabolism*
chemical_list: D000701:Analgesics, Opioid; D001786:Blood Glucose; D006146:Guanidines; D017480:Receptors, sigma; D006220:Haloperidol; C050232:1,3-ditolylguanidine; D010423:Pentazocine