Opiate and digitalis receptor assays distinguish between neuroexcitant and inactive organochlorines and between anesthetics and convulsants.
Specific binding of [3H]naloxone to rat brain tissue in vitro was inhibited by the excitant organochlorinated insecticides (OCI), by ether (E) and octanol (OCT), and by the convulsant indoklon (IND) and its anesthetic isomer, isoindoklon (ISO). In the presence of 100 mM NaCl the inhibition of naloxone binding by E, OCT and ISO was greatly potentiated, whereas that by OCI and IND was attenuated. KCl (100 mM) was equally effective as NaCl on the action of anesthetics, but the effect of the excitant drugs was, in contrast to NaCl, unaffected by KCl. Specific binding of [3H]ouabain in the absence of Na, was depressed by anesthetics and enhanced by neuroexcitants. In the presence of NaCl, which by itself inhibits ouabain binding to brain, both anesthetics and excitants enhanced ouabain binding. DDE, a non-insecticidal analog of DDT, and the dimethyl derivative of the OCI, lindane, were inactive in the receptor assays. These observations point to a unique isolated system which responds consistently to anesthetic agents as a class and, in a different way, to neuroexcitant compounds.
D000777:Anesthetics / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects*; D003292:Convulsants / Q000494:pharmacology*; D003634:DDT / Q000494:pharmacology; D003633:Dichlorodiphenyl Dichloroethylene / Q000494:pharmacology; D004986:Ether / Q000494:pharmacology; D005481:Flurothyl / Q000494:pharmacology; D001556:Hexachlorocyclohexane / Q000494:pharmacology; D007306:Insecticides / Q000494:pharmacology*; D009270:Naloxone / Q000378:metabolism; D000442:Octanols / Q000494:pharmacology; D051381:Rats; D011955:Receptors, Drug / Q000187:drug effects*; D011957:Receptors, Opioid / Q000187:drug effects*; D000254:Sodium-Potassium-Exchanging ATPase; D005466:Fluorocarbons
D000777:Anesthetics; D003292:Convulsants; D003634:DDT; D003633:Dichlorodiphenyl Dichloroethylene; D004986:Ether; D005481:Flurothyl; D001556:Hexachlorocyclohexane; D007306:Insecticides; D009270:Naloxone; D000442:Octanols; D011955:Receptors, Drug; D011957:Receptors, Opioid; D000254:Sodium-Potassium-Exchanging ATPase; C027082:digitalis receptor; C030560:iso-Indoklon; D005466:Fluorocarbons