Muscarinic receptor in house fly brain and its interaction with chlorobenzilate

Shaker, N.; Eldefrawi, Amira T.

doi:10.1016/0048-3575(81)90030-4

Cited by 34 publications

(4 citation statements)

References 21 publications

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“…d-Tubocurarine, a specific vertebrate nicotinic antagonist, did appear to inhibit a proportion of [N-methyl-3H]scopolamine binding at high concentrations in the cockroach. Similar findings of inhibition of [3H]quinuclidinyl benzilate binding by relatively low concentrations of dtubocurarine have also been observed in several other invertebrate preparations [6,7,23] However, d-tubocurarine remains several orders of magnitude less active on invertebrate muscarinic receptors than conventional muscarinic ligands.…”

Section: Discussionsupporting

confidence: 77%

[N‐Methyl‐³H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana

Lummis¹,

Sattelle²

1986

Arch Insect Biochem Physiol

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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.

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Section: Discussionsupporting

confidence: 77%

[N‐Methyl‐³H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana

Lummis¹,

Sattelle²

1986

Arch Insect Biochem Physiol

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“…The very high density of [3H]QNB binding sites in TG preparations is closer in magnitude to that of muscarinic AChRs in regions of mammalian brain (Kloog et al, 1979;Salvaterra and Foders, 1979) than to binding site concentrations found in other invertebrate preparations studied, including fly head (Dudai and Ben-Barak, 1977;Jones and Sumikawa, 1981;Shaker and Eldefrawi, 1981) and cockroach nerve cord (Lummis and Sattelle, 1983) homogenates. In contrast, the affinity constant (apparent KD of 5-10 nM) obtained by two independent kinetic methods is very close to that recently described for the cockroach preparation, but is more than an order of magnitude lower than that calculated for most vertebrate neuronal and nonneuronal classes of muscarinic AChRs (e.g., Yamamura and Snyder, 1974;Galper et al, 1977) or for [3H]QNB binding sites in fly head homogenates (Dudai and Ben-Barak, 1977;Jones and Sumikawa, 1981).…”

Section: [3h]qnb Binding Sitesmentioning

confidence: 77%

Muscarinic and Nicotinic Cholinergic Binding Sites in the Terminal Abdominal Ganglion of the Cricket (Acheta domesticus)

Meyer

Reddy

1985

Journal of Neurochemistry

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Cricket (Acheta domesticus) terminal abdominal ganglia (TG) contain high concentrations (approximately 2 pmol/mg protein) of muscarinic and nicotinic cholinergic binding sites, based on the capacity of TG to bind specifically the labelled ligands L-[3H]quinuclidinyl benzilate ([3H]QNB) and [125I]alpha-bungarotoxin ([125I]alpha-BGT) with high affinity. For both ligands, binding is saturable and reversible. Competitive displacement experiments indicate that the [3H]QNB and [125I]alpha-BGT binding sites probably represent pharmacologically distinct classes of putative TG acetylcholine receptors (AChRs). Results from physiological recording and autoradiographic localization experiments demonstrate that a portion of the putative nicotinic AChRs is localized in synaptic regions of the well-characterized cercal sensory-giant interneuron pathway in the TG, where they are likely to serve as functional synaptic AChRs. Unlike nicotinic ligands, muscarinic agents do not appear to be pharmacologically active in this pathway. Therefore, in the insect CNS, putative muscarinic and nicotinic AChRs coexist at high density, but can be pharmacologically distinguished from one another on the basis of criteria derived from both ligand binding and physiological methods.

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“…4 On the other hand, there is minimal information on the potential of the mAChR as a viable target site for insect control. 5,6 These receptors belong to a di †erent superfamily of proteins, generally referred to as G-coupled proteins. Unlike the nAChR, muscarinic receptors do not contain integral ion channels but rather transduce their signals intracellularly via second messengers (such as cAMP) through interactions with G-coupled proteins.…”

Section: Introductionmentioning

confidence: 99%

Muscarinic Agonists as Insecticides and Acaricides

1997

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: A series of known agonists of the mammalian muscarinic receptor were prepared and evaluated for their insecticidal potential. It was discovered that pests such as Nilaparvata lugens (brown planthopper), Nephotettix cincticeps (green leafhopper), T etranychus urticae (two-spotted spider mite) and Aphis gossypii (cotton aphid) were particularly sensitive to most of these compounds. Several analogs proved to be extremely active, surpassing commercial standards in some of the laboratory bioassays. These compounds exhibited a range of potencies for the insect (Musca) muscarinic receptor. Addition of GTP signiÐ-cantly reduced the affinity of the most potent analog for the Musca mAChR, indicating the compound functions as an agonist in insect tissue. Regression analysis indicated that signiÐcant relationships exist between displacement of [3H]QNB at the Musca muscarinic receptor and whole organism toxicity to three insect and one mite species. The results suggested that the insect muscarinic receptor represents a viable target site for insecticidal action.

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Muscarinic receptor in house fly brain and its interaction with chlorobenzilate

Cited by 34 publications

References 21 publications

[N‐Methyl‐³H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana

[N‐Methyl‐³H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana

Muscarinic and Nicotinic Cholinergic Binding Sites in the Terminal Abdominal Ganglion of the Cricket (Acheta domesticus)

Muscarinic Agonists as Insecticides and Acaricides

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Muscarinic receptor in house fly brain and its interaction with chlorobenzilate

Cited by 34 publications

References 21 publications

[N‐Methyl‐3H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana

[N‐Methyl‐3H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana

Muscarinic and Nicotinic Cholinergic Binding Sites in the Terminal Abdominal Ganglion of the Cricket (Acheta domesticus)

Muscarinic Agonists as Insecticides and Acaricides

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[N‐Methyl‐³H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana

[N‐Methyl‐³H]Scopolamine binding sites in the central nervous system of the cockroach Periplaneta americana