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1.
The formamidines chlordimeform, demethylchlordimeform (DCDM), amitraz and BTS-2727l were tested for their respective abilities to inhibit [3H]mianserin binding in membrane preparations of cockroach brain and, in the same tissue, to stimulate octopamine-sensitive receptors coupled to adenylate cyclase. Analysis of [3H]mianserin binding indicated negative cooperativity between two binding sites with respective Kd and Bmax values of 3.82 mM and 0.886 pmol (mg protein)?1 for a high-affinity site and 218 nM and 13.56pmol (mg protein)?1 for a low-affinity site. DCDM, BTS-27271 and amitraz inhibit [3H]mianserin binding with IC50 values similar to those obtained with octopamine and the μ-adrenergic antagonist, phentolamine, whereas chlordimeform is a poor competitor for the binding sites. Similarly DCDM, BTS-27271 and amitraz elevate cyclic AMP production in brain membrane preparations in a dose-dependent manner with Ka values of 0.32 uM, 1.5 uM and 3.4 uM respectively, whereas chlordimeform was again without effect. The formamidine-mediated responses were fully additive with the evaluation of cyclic AMP obtained using the maximal concentration of dopamine but not with octopamine-mediated increases; thus the formamidine effects appear to be expressed through partial agonism of octopamine receptors that are coupled to adenylate cyclase.  相似文献   

2.
Application of the formamidine pesticides chlordimeform (CDM) and desmethylchlordimeform (DCDM) induced the release of hyperlipemic hormone from the isolated corpus cardiacum (CC) of the locust, Locusta migratoria. Pretreatment of locusts with reserpine (10 μg/locust) had no effect on formamidine-induced release of the hyperlipemic hormone. The action of CDM and DCDM on isolated CC was blocked by the α-adrenergic-receptor blocker, phenoxybenzamine, but not by the β-adrenergic blocker, propranolol. These formamidines also potentiated the release of the hyperlipemic hormone induced by electrical stimulation of nervus corpus cardiacum II (NCC II). The evidence presented in this paper indicates that, in locusts, CDM and DCDM, or their metabolites, act on postsynaptic aminergic (octopamine) receptors in the glandular lobe of the CC, inducing the release of hyperlipemic hormone.  相似文献   

3.
The relative toxicity (μg a.i. g?1 body wt) of the formamidine insecticide chlordimeform (CDM) and the triazapentadiene insecticide amitraz was examined in two species of noctuid moth Spodoptera littoralis and Heliothis virescens. When applied topically, there was an unexpected and marked difference in the toxicity of CDM base and its hydrochloride to adults of both species, the salt being appreciably more toxic. For H. virescens at least, this difference in toxicity could not be explained by differences in penetration. This trend was reversed for larval instars of S. littoralis; while there was relatively little difference in the toxicity of the base to adult and larval stages, the salt was at least 1000-fold more toxic to adults than to larvae. N1-Demethylchlordimeform (DCDM) was the only metabolite of CDM to show biological activity against either species, but was much less toxic than the parent compound. Amitraz was far less toxic than either CDM or DCDM; like the CDM salt, it appeared to be more toxic to adult than larval stages of S. littoralis. Application of piperonyl butoxide significantly increased the toxicity of the CDM salt, DCDM and amitraz to adult H. virescens, the synergist being particularly effective with DCDM and amitraz. In contrast, piperonyl butoxide had no significant effect on the toxicity of DCDM, and slightly antagonised the toxicity of DCDM to fourth-instar larvae of S. littoralis.  相似文献   

4.
Dihydrooxadiazines are structural analogs of octopamine and were compared with octopamine for their ability to compete with [3H]dihydroergocryptine ([3H]DHE) for binding sites on DHE-sensitive receptors, to stimulate adenylate cyclase activity in nervous system homogenates of Periplaneta americana L., and to modulate the action of the peptide proctolin on the oviducal muscles of Locusta migratoria L. [3H]DHE binding was inhibited by low concentrations (μM range) of octopamine, phentolamine, N-demethylchlordimeform (DCDM) and several dihydrooxadiazines. The tested dihydrooxadiazines acted as aminergic agonists in stimulating cyclic AMP production in cockroach nervous system homogenates and did not show additive effects with octopamine, whereas additivity was observed with 5-hydroxytryptamine. The relative potency of octopaminergic antagonists, including mianserin, cyproheptadine, phentolamine, and gramine, to block octopamine-mediated elevation of cyclic AMP production was similar to the rank-order potency of the same antagonists to inhibit dihydrooxadiazine-mediated elevation of cyclic AMP production. Octopamine, 2-(4-bromophenyl)-5,6-dihydro-4H-1,3,4-oxadiazine (4-Br-PDHO), and 8-Br-cyclic AMP caused increased phosphorylation of proteins that are phosphorylated by exogenously added cyclic AMP-dependent protein kinase. These results indicate that the dihydrooxadiazine-induced rise in cyclic AMP levels in homogenates of the cockroach nervous system results directly in activation of an endogenous cyclic AMP-dependent protein kinase. 4-Br-PDHO behaved similarly to octopamine in modulating the action of proctolin-induced contractions in locust oviducal muscles. These observations suggest that dihydrooxadiazines act as octopamine agonists and have an octopaminergic action in modulating the action of proctolin. Thus, it is proposed that dihydrooxadiazines exert at least part of their insecticidal and miticidal actions through interaction with the octopaminergic system.  相似文献   

5.
Membrane potential and voltage clamp measurements of the responses to octopamine, dopamine, O-acetylcholine, and the formamidine derivatives chlordimeform (CDM) and N1-demethylchlordimeform (DCDM) have been made on identified central neurones of Helix aspersa. DCDM and CDM were agonists on both the inhibitory and excitatory octopamine receptors on these neurones but were less potent than octopamine. The direct inhibitory effect of DCDM was antagonised by both phentolamine and cyproheptadine. DCDM was also found to antagonise the effects of octopamine, dopamine and O-acetylcholine on these neurones. The pA2 values for DCDM against dopamine and O-acetylcholine were 5.2 (±0.1) and 5.35 (±0.15), respectively. The pA2 value=log[DR-(1/I)], where I is the concentration of the antagonist, and DR=dose ratio =A2/A1; A1 is the dose of agonist required to produce 50% of the maximum response, and A2 is the dose of agonist needed to produce the same degree of response in the presence of the antagonist. It is concluded that DCDM and CDM act specifically on the octopamine receptors of H. aspersa central neurones, both as agonists and antagonists. The antagonist effect of DCDM against dopamine receptors is probably non-specific.  相似文献   

6.
The action of insecticides on the spontaneous electrical activity of neurohemal tissue in the stick insect, Carausius morosus, has been studied using extracellular electrodes. The pyrethroid, permethrin, causes a massive increase in the frequency of the spontaneously generated action potentials at concentrations between 5 × 10?5 and 5 × 10?8M. Concentrations as low as 5 × 10?11M are still effective in producing bursting activity.DDT, at concentrations between 5 × 10?5M and 5 × 10?6M, produces an overall increase in activity although the bursting activity is less violent than that shown with permethrin. DDT, 5 × 10?7M, is ineffective at altering the resting pattern.Carbaryl and coroxon cause a transitory increase in electrical activity at 1 × 10?4M, but are ineffective at 1 × 10?5M.It is concluded that insecticides could have a direct effect upon the neurohormonal balance in insects.  相似文献   

7.
Amitraz is a pesticide targeting the octopaminergic receptors. In a previous study, octopamine, a biogenic amine, was found to induce a biphasic effect on the honeybee heart, inhibition at low concentrations and excitation at high concentrations. Furthermore, the honeybee heart was found to be far more sensitive to octopamine compared to other insect hearts. The objective of the present study was to investigate the effects of amitraz on the electrical and mechanical properties of the honeybee heart ex vivo and on the heart rate in vivo. In ex vivo conditions, amitraz at 10−12 M caused a significant inhibition in the mechanical (p < 0.05, n = 4) and electrical properties (p < 0.05, n = 4). Higher concentrations such as 10−9 and 10−6 M induced a biphasic effect, with total inhibition for 7.86 ± 1.26 min (n = 7), followed by strong excitation of spontaneously-generated contractions (n = 7). The initial elimination of heart activity was caused by strong hyperpolarization, while the subsequent excitation was caused by a depolarization in the membrane potential of pacemaker cells at 10−9 M (n = 8). In the in vivo experiments, abdominal injection or oral application of 0.20 ng of amitraz per bee induced a persistent increase of 134.28 ± 4.07% (p < 0.05, n = 4) in the frequency of the cardiac action potentials. The above responses clearly show that the heart of the honeybee is extremely vulnerable to amitraz, which is nevertheless still used inside beehives, ostensibly to “protect” the honeybees against their main parasite, Varroa destructor.  相似文献   

8.
Formetanate, a formamidine-type pesticide, and U-40481 (N-methyl-N′-2,4-xylylformamidine), a metabolite of amitraz, also a formamidine pesticide, contract the rabbit central ear artery with their maximal contractions being 22 ± 8% and 49 ± 6% of norepinephrine contractions, respectively. Maximal contractions were obtained with 10?3M formetanate and 10?4M U-40481, and cumulatively added higher concentrations caused a decrease in tension from that maximum. Their contractions were antagonized by 10?6M and 3 × 10?6M phentolamine. U-40481 reversibly antagonized contractions induced by serotonin, norepinephrine, and histamine, and to some extent potassium. Formetanate had little antagonist activity. Neither compound altered the resting rate of washout of radioactivity from [3H]norepinephrine preloaded strips. Both reduced electrically induced release, which may be related to local anesthetic-like actions on sympathetic neurones. Thus both compounds are partial agonists at the α-adrenergic receptor, and reduce electrically induced norepinephrine release, and U-40481 antagonizes contractions induced by certain other vasoactive agents.  相似文献   

9.
The pesticides, chlordimeform and amitraz, and their metabolites, demethylchlordimeform, N1-(2,4-dimethylphenyl)-N-methylformamidine, and 2,4-dimethylformanilide, are effective at concentrations as low as 3 μM in raising the firing rate of endogenously active neurosecretory fibres in the isolated neurohaemal organs of Carausius morosus. Molecules such as bunamidine and cetrimide, with cationic detergent properties, produced sporadic bursting which did not elevate the overall firing rate to any great extent. Indeed, bunamidine could induce complete block of action potentials at concentrations as low as 30 μM. The local anesthetics, procaine, lidocaine, and benzocaine, do not induce block of activity at least up to a level of 1 mM. They have no effect at concentrations lower than 100 μM. Between 100 μM and 1 mM lidocaine and benzocaine produce a small increase in firing rate. Procaine produced a pronounced increase in the frequency of firing. The phenolic amines, octopamine, synephrine, and tyramine, markedly increased electrical activity. The catecholamines, dopamine, noradrenaline, and adrenaline, by contrast, only produced a weak excitation. Neither α- nor β-adrenergic blocking agents were effective in antagonizing the electrical activity induced by chlordimeform or phenolic amines until relatively high concentrations of about 1 mM were used. Chlordimeform was able to induce high-frequency bursts from sense organs associated with the epidermis and body-wall musculature in larvae of Musca domestica and Calliphora erythocephala. Octopamine did not induce any similar bursting activity in these sense organs. These results are discussed in relationship to current views on the mode of action of the N-aryl amidines. It is concluded that the excitatory effects of these compounds upon neurohaemal organs and sense organs are more likely to result from a direct action upon voltage sensitive channels of the nerve membranes, rather than by an effect mediated by interactions with octopamine receptors.  相似文献   

10.
By employing intracellular electrodes on the 6th abdominal ganglion, Cartap hydrochloride 10?5M caused in all experiments a block of the provoked stimulus transmission and a decrease of the cell membrane resting potential; the giant fiber conduction was not affected. In the experiments with extracellular electrodes Cartap 10?5M provoked a marked increase of the spontaneous activity followed by block which partially disappeared after washing. The same effects were obtained on spontaneous activity when Cartap 10?5M was used on the denervated 6th abdominal ganglion and in experiments conducted at 0 Ca2+ or at 20 mM Mg2+. Cartap 10?5M did not affect the response to direct or indirect stimulation of cockroach neuromuscular preparation. These results tend to confirm that Cartap affects the postsynaptic region of the ganglionic nervous junction. The possible cause of the resting potential decrease is also discussed.  相似文献   

11.
In apterous adults of the spirea aphid, Aphis citricola van der Goot, the optimum conditions for determining acetylcholinesterase (AChE) activity consist of reaction mixture of 0.1 M phosphate buffer (pH 7.5), 10?3M acetylthiocholine (ASCh), and enzyme extract equivalent to 80 ± 3 μg protein incubated for 15 min at 30°C. The Km value for ASCh (6.7 × 10?5M) was much lower than that of butyrylthiocholine (BuSCh) (1.25 × 10?2M). The enzyme activity was almost completely inhibited by 10?6M paraoxon or 10?5M eserine and was 84% inhibited by 10?5M BW284C51 (a specific AChE inhibitor). DTNB was found to inhibit the enzyme activity and was therefore added at the end of the reaction. AChE activity of A. citricola was inhibited in vitro and in vivo by dimethoxon > dimethoate, and aldicarb sulfoxide > aldicarb > aldicarb sulfone. The in vivo effect correlates well with the toxicity level of the various toxicants. A neurotoxicity index which combines both mortality and in vivo inhibition of the aphid AChE activity is suggested as a measure for determining the toxicity of organophosphorus and carbamate compounds toward aphids.  相似文献   

12.
At concentrations near 2 × 10?4M, barban, chlorpropham, and phenmedipham are inhibitors of the electron transfer in potato and mung bean mitochondria. The inhibition seems to be localized in the flavoprotein region. It affects preferentially the exogenous NADH dehydrogenation, in potato mitochondria (I50, 10?4M). Succinate dehydrogenation is less inhibited. At noninhibiting concentrations, the studied carbamates cannot uncouple the oxidative phosphorylations. Photosynthesis is completely inhibited by 2.10?7M phenmedipham, 5 × 10?5M barban, and 2 × 10?4M chlorpropham. The inhibition takes place at the PS II level. Moreover, barban and chlorpropham are uncouplers of the photophosphorylations for concentrations between 5 × 10?5 and 5 × 10?4M. The effects observed on mitochondrial respiration can also be found on respiration of Acer cultured cells. The effects on isolated chloroplast photosynthesis are also observed for slightly higher concentrations on cultured Chlorella and on pea and oat leaf fragments.  相似文献   

13.
The action of avermectin was studied in the leg muscle and the central nervous system of the American cockroach, Periplanata americana L. Avermectin at a low concentration (10?7M) causes a failure of the leg muscles to respond to external stimuli within 30 min without affecting the magnitude of contraction. Avermectin was found to stimulate Cl? uptake by the leg muscles within 4 min at 10?7M. The threshold concentration to cause such stimulation was on the order of 10?8M. This stimulatory action could be antagonized by picrotoxinin (10?4M) and to a lesser extent by bicuculline methiodide (10?4M). The phenomenon is observable under both Na+-free and K+-free conditions. It was concluded that the action of avermectin is to open the chloride channel on the plasma membrane. This action of avermectin does not seem to be mediated through GABA, GABA receptors, diazepine receptors, or picrotoxinin receptor in this insect species, and therefore suggests that avermectin directly attacks the chloride channel proper both in the central nervous and the neuromuscular systems.  相似文献   

14.
The effects of chlordimeform on rectus abdominis muscle of frog were investigated. Chlordimeform (10?3M) caused a slow contraction, and at lower concentration (10?5–10?3M) it inhibited the acetylcholine-induced contraction in noncompetitive manner. When chlordimeform was applied to the muscle of Rana catesbiana, K+-induced contraction was also inhibited in noncompetitive manner. Whereas it had no effect on caffeine-induced contraction.Chlordimeform-induced contraction was not affected by respective addition of d-tubocurarine (10?4M), procaine (10?3M), or eserine (0.3 mM), which results were same as that of K+-induced contraction. Chlordimeform, at lower concentration (10?5–10?3M), inhibits the acetylcholine- and K+-induced contractions probably owing to depression of not only the sensitivity of endplate but also the excitability of cell membrane.  相似文献   

15.
Deltamethrin and NRDC 157, pyrethroid insecticides that produce different poisoning syndromes in mammals, enhanced veratridine-dependent, sodium channel-mediated 22Na+ uptake in mouse brain synaptosomes. Concentrations producing half-maximal enhancement were 2.5 × 10?8M (deltamethrin) and 2.2 × 10?7M (NRDC 157). This effect was stereospecific: The nontoxic 1S enantiomers had no significant effect on veratridine-dependent activation. At high deltamethrin concentrations, enhancement was maximal at 5 × 10?5?1 × 10?4M veratridine. Pyrethroid enhancement was completely blocked by 5 × 10?6M tetrodotoxin, and neither pyrethroid affected 22Na+ uptake in the absence of veratridine at concentrations up to 1 × 10?5M. The relative potencies of deltamethrin and NRDC 157 in the synaptosomal sodium channel assay agree well with their relative acute toxicities to mice when administered by intracerebral injection. These findings demonstrate that pyrethroids exemplifying both characteristic poisoning syndromes are potent, stereospecific modifiers of sodium channel function in mammalian brain.  相似文献   

16.
The calcium entry blockers sodium nitroprusside (10?2M) and sodium pentobarbital (5 × 10?3M) had different effects on high-potassium-induced and Frescon-induced contractures in a smooth and a cross-striated muscle of the snail Lymnaea stagnalis. This suggests that Frescon causes an increase in sarcolemmal calcium permeability by a mechanism which is different from that utilized by high extracellular potassium.  相似文献   

17.
The effect of trifluralin on the growth, oxygen uptake, and adenosine phosphates level of carrot (Daucus carota L.) callus tissue was determined over a period of 18 days after subculture. The herbicide (10?4 and 10?5M) reduced fresh weight gain significantly; the reduction was less with lower trifluralin concentrations. Dry weight accumulation was not inhibited until after Day 6 of the test period and thereafter was reduced by all concentrations tested. Oxygen consumption was inhibited by trifluralin (10?4 and 10?5M) throughout the test period. Concentrations of 10?6.10?7, and 10?8M produced variable effects. The response profile of O2 consumption in the presence of dinitrophenol was different from that of trifluralin. Analysis of adenosine phosphates level gave no clear response trend. Energy charge values of 0.7 to 0.85 were obtained for untreated tissue. Trifluralin had no effect on energy charge until Day 9 (10?4M) and after Day 15 (all concentrations).  相似文献   

18.
DDT inhibits the ATPase activity of the intact eel electroplaque. At a concentration of 10?5M, DDT inhibited 46% of the total ATPase activity, and 10?4M DDT inhibited 62% of the total ATPase activity and 62% of the ouabain-sensitive ATPase activity. The latter concentration of DDT reduced the rate of Na efflux from intact electroplaques and slowed the rate of recovery of the membrane potential following a large depolarization produced by carbamylcholine application. Repetitive direct stimulation of the innervated membrane at 10 Hz during the application of 10?4M DDT produced a significant irreversible depolarization. Ouabain, 10?4M, produced similar effects. The possible role of the inhibition of active NaK transport in producing the symptoms of DDT poisoning is discussed.  相似文献   

19.
The binding behavior of mercuric chloride (HgCl2), phenylmercuric acetate (PMA), and ethylmercuric chloride (EMC) to the spinach chloroplasts in relation to the inhibition of the Hill reaction was studied at pH 6.8 and 7.8 using 203Hg labeled compounds. The pH of the reaction medium did not influence the amount of mercury binding of the chloroplast at various mercurial concentrations, but it altered the inhibition curve of the Hill reaction. Between 0–1 × 10?5M the binding of Hg2+ and EMC were similar and increased linearly with the concentration, while the binding of PMA was similar to the binding of Hg2+ only at a concentration below 4 × 10?6M and was less when the concentration was above 4 × 10?6M. However, the inhibition of the Hill reaction by these mercury compounds was quite different; at pH 7.8, the I50 values for Hg2+, PMA, and EMC were 5 × 10?6, 2.5 × 10?6, and 2.5 × 10?6M, respectively, while at pH 6.8, these values were 4 × 10?6, 4 × 10?5, and 2 × 10?4M, respectively. The differential block of electron flow by the mercury compounds at pH 6.8 and 7.8 was further confirmed by electron spin resonance study.  相似文献   

20.
Over a concentration range of 5.0 × 10?6?7.5 × 10?4M, the selective herbicide difenzoquat (1,2-dimethyl-3,5-diphenyl-1H-pyrazolium) caused more pronounced inhibition of potassium ion (K+) absorption by excised seedling roots of susceptible wild oat (Avena fatua L.) compared to those of tolerant barley (Hordeum vulgare L. cv. Bonanza) or wheat (Triticum aestivum L. cv. Neepawa). At 2.5 × 10?5M difenzoquat, the relative inhibition of K+ (86Rb) absorption by wild oat root segments inceased from 30% with a 10-min uptake period to 75% with an uptake period of 90 min, whereas no inhibition at all was evident for wheat root segments even after a 90-min exposure to the herbicide. An ion efflux compartmental analysis procedure demonstrated that difenzoquat did not affect the passive permeability properties of the plasma membrane of wild oat root cells. The experimental findings indicated that difenzoquat interfered directly with the process of active ion transport across the plasma membrane of root cells.  相似文献   

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