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γ-Aminobutyric Acid Receptor Ionophore Complexes: Differential Effects of Deltamethrin, Dichlorodiphenyltrichloroethane, and Some Novel Insecticides in a Rat Brain Membrane Preparation (1987)

Lummis, Sarah C. R. ; Chow, Shirley Chen ; Holan, George ; [et al.]

Oxford, UK : Blackwell Publishing Ltd

Journal of neurochemistry 48 (1987), S. 0

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ISSN: 1471-4159

Source: Blackwell Publishing Journal Backfiles 1879-2005

Topics: Medicine

Notes: Abstract: The binding of [35S]t-butylbicyclophosphorothionate ([35S]TBPS), a γ-aminobutyric acid (GABA)-activated chloride ionophore ligand; [3H]diazepam, a benzodiazepine agonist; and [3H]muscimol, a GABA receptor probe, were used to assess the effects at 100 μM of deltamethrin, dichlorodiphenyltrichloroethane (DDT), and three experimental insecticides—a DDT-pyrethroid hybrid, GH414 (cycloprothrin), and two DDT-analogues, GH266 and GH149 (EDO), on GABA receptor ionophore complexes in a rat brain membrane preparation. GH266 and GH149 were found to inhibit a greater percentage of [35S]TBPS binding than the same concentration of deltamethrin or DDT, although GH414 had little effect. GH266 and GH149 enhanced [3H]diazepam binding by nearly 200%, in contrast to the inhibitory effects of deltamethrin, DDT, and GH414. GH266 and GH149 also caused a dramatic enhancement of [3H]muscimol binding, 367 and 236% of control, respectively, whereas DDT and deltamethrin caused only a moderate enhancement. The effects of the insecticides on binding affinity and density were examined for each of the ligands. The results show a differential interaction of the insecticides on the various ligand binding sites.

Type of Medium: Electronic Resource

URL: http://dx.doi.org/10.1111/j.1471-4159.1987.tb05571.x

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[N-Methyl-3H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana (1986)

Lummis, Sarah C. R. ; Sattelle, David B.

New York, NY [u.a.] : Wiley-Blackwell

Archives of Insect Biochemistry and Physiology 3 (1986), S. 339-347

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ISSN: 0739-4462

Keywords: Muscarinic acetylcholine receptors ; cockroach CNS ; [N-methyl-3H]scopolamine ; Chemistry ; Food Science, Agricultural, Medicinal and Pharmaceutical Chemistry

Source: Wiley InterScience Backfile Collection 1832-2000

Topics: Biology

Notes: The binding of [N-methyl-3H]scopolamine to a cockroach nerve cord preparation has been investigated. Specific [N-methyl-3H]scopolamine binding was found to be saturable and of high affinity (Kd = 13.9 nM). Muscarinic ligands were found to displace [N-methyl-3H]scopolamine binding more effectively than nicotinic ligands. The distribution of these [N-methyl-3H]scopolamine binding sites was examined in the metathoracic ganglion at the light microscope level by autoradiographical techniques. Specific binding was found to be localized to distinct regions of the neuropile. This pattern showed certain similarities to that seen when the ganglion was stained for acetylcholinesterase, suggesting a functional role for these insect muscarinic acetylcholine receptors.

Additional Material: 3 Ill.