Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.1.1.7 (acetylcholinesterase)
28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Behavioral effects of nicotine and cytisine, and the cholinesterase inhibitors physostigmine and 9-amino-1,2,3,4-tetrahydroacridine (THA), administered intrathecally (IT) at the lumbar level in the rat have been evaluated. Antinociceptive dose relationships were established using the tail immersion test. Total activity, locomotion and rearing were also measured in computerized test boxes. The nicotinic receptor antagonist, mecamylamine, and the muscarinic receptor antagonist, atropine, were used to study the selectivity of the effects. Physostigmine and THA significantly decreased total activity, locomotion and rearing as compared to control animals. The motor effects of physostigmine were completely antagonized only partly. Mecamylamine had no antagonistic effect. Nicotine did not affect any activity parameter. Cytisin reduced total activity and locomotion 1-6 min after dose. IT physostigmine, 15 micrograms, increased tail immersion latency for 30 min. No significant increase in response latency in this test was observed after the IT administration of nicotine or THA, whereas cytisine elicited a small increase. The IT administration of THA, nicotine and cytisine was also associated with gnawing, vocalization and hyperactivity and in the case of THA, diarrhoea. These effects were blocked by mecamylamine. Physostigmine antinociception as well as the behavioral effects including total activity, locomotion and rearing caused by physostigmine and by THA are most probably due to an action on spinal muscarinic receptors. Nicotinic receptors do not seem to be involved in spinal antinociception. Some aversive behavioral effects caused by the IT administration of nicotinic receptor agonists could, however, be attenuated by the spinal administration of the antagonist mecamylamine, which may indicate the involvement of nicotinic receptors in afferent sensory transmission.
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PMID:Behavioral effects after intrathecal administration of cholinergic receptor agonists in the rat. 232 Jul 7

Repeated application of hexachlorocyclohexane (HCH; 50 and 100 mg/kg) and malathion (200 and 400 mg/kg) alone or in combination daily for 30 days on the skin of male guinea pigs caused mild to severe signs of toxicity and death of animals. The experimental animals exhibited tremor, dyspnea, salivation, convulsion, diarrhea and paralysis of the limbs. These were associated with significant biochemical and morphological changes in skin, liver, kidney and testes. The inhibition of acetylcholinesterase appeared highly significant in the combined treatment, but was not suggestive of any HCH and malathion potentiation. The highest level of HCH residue was seen in fatty tissue after low dose treatment. This was in contrast to the high level seen in liver after larger doses of HCH. This study suggests that HCH and malathion did not elicit any potentiation effects in the parameters monitored and at the doses tested.
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PMID:Interaction of hexachlorocyclohexane and malathion in male guinea pigs after repeated dermal application. 243 88

Healthy camels were experimentally infected with Trypanosoma evansi and then treated with isometamidium chloride (samorin) at single intravenous doses of 0.5 or 1.0 mg/kg. Five to 10 min after the drug administration, the camels at both dosages showed lacrimation, salivation, trembling, restlessness, frequent urination and defecation, followed by diarrhea. Moreover, the camels at the higher dose showed an unsteady gait for about an hour with hindleg weakness and walking backward. The animals fell to the ground, laid on their sides, and bent their necks into an "S" shaped curve. Three hours after the drug administration all the animals stood up and remained quiet. The treatment increased the concentration of plasma ammonia and total protein. No significant change was found in the plasma bilirubin concentration. Two hours after treatment, the activity of plasma cholinesterase was significantly reduced. The enzyme activity recovered 24 h after drug administration, but was still significantly below the control value. The treatment did not produce statistically significant changes in the hemogram of the infected camels. The results suggest that the drug should not be used clinically against T evansi infection due to its low margin of safety. If the drug is to be used at all in camels, pretreatment with an anticholinergic agent might be considered.
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PMID:Some observations on the toxicosis of isometamidium chloride (samorin) in camels. 377 85

Thirty-eight 7-week-old white leghorn chickens of two strains (high and low antibody response to sheep erythrocytes) were divided into groups for exposure to high and low levels of social stress. They were then challenged orally with a toxic dose of the organophosphate insecticide malathion (250 mg/kg body weight) and evaluated 60 min later for muscarinic signs (diarrhea, lacrimation, respiratory secretions), nicotinic signs (muscle weakness), plasma cholinesterase activity, and brain acetylcholinesterase activity. A significant correlation was shown between clinical and biochemical indices of organophosphate toxicity. The correlation between social stress and malathion toxicity was less well defined. Chickens with low antibody response preexposed to high social stress were most resistant to organophosphate toxicity.
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PMID:Effects of social stress on the toxicity of malathion in young chickens. 381 4

The acute effects of diisopropylfluorophosphate (DFP) were assessed in DBA/2Ibg, C57BL/6Ibg and C3H/2Ibg mice. The DFP was administered by intraperitoneal injection in saline. Brain acetylcholinesterase (AChE) activity was maximally inhibited within 5 min after injection. All mice showed signs of organophosphate intoxication including salivation, lacrimation, diarrhea, respiratory distress, tremor and, at high doses, seizures. The C57BL mice were most susceptible to these effects of DFP. The LD50 values for DFP were 8.0, 7.6, and 6.8 mg/kg for male DBA, C3H, and C57BL mice, respectively. The LD50 values for females were nearly the same. Body temperature and brain AChE activity decreased in a dose-dependent manner following injections of DFP of 3.17, 4.22, 5.28, and 6.33 mg/kg. Maximum temperature depression occurred 2 hours after DFP administration; by 24 hours temperatures had returned to normal except for C57BL mice treated with the highest dose of DFP. The C57BL strain was most susceptible to the DFP-induced hypothermia, the C3H strain was the most resistant, and the DBA strain was intermediate. Maximum temperature depression and residual AChE activity, as measured 24 hours after injection, were linearly related. These strain differences do not seem to be explained easily by a differential inhibition of AChE activity.
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PMID:Genetically determined differences in acute responses to diisopropylfluorophosphate. 399 71

1. Daily i.p. administration, for eight days, of the cholinesterase inhibitor disulfoton to rats produced mild to moderate signs of intoxication (tremors, incontinence and diarrhoea) but no deaths.2. Segments of ileum taken from the treated rats were subsensitive to carbachol but the vas deferens and the uterus did not exhibit any change in sensitivity to carbachol.3. The sensitivity to acetylcholine was increased in the ileum and vas deferens but not in the uterus.4. Acetylcholinesterase activity was 60-70% inhibited in all three tissues.
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PMID:Response of the rat ileum, uterus and vas deferens to carbachol and acetylcholine following repeated daily administration of a cholinesterase inhibitor. 476 90

In the United States, the drugs most commonly used to treat peptic ulcer disease are antacids and the H2-receptor antagonists cimetidine and ranitidine. Other available agents include anticholinergics and the coating agent sucralfate. Investigational drugs such as colloidal bismuth, carbenoxolone, prostaglandins, the tricyclic compound pirenzepine, and substituted benzimidazoles are not available for use in the United States. Most of the commercially available and investigational compounds have similar efficacy; therefore the optimal drug may be the one associated with the fewest adverse effects and the most convenient dosing regimen. Cimetidine causes a small number of adverse effects, including neuropsychiatric disorders, gynecomastia, impotence, loss of libido, elevation of serum creatinine and serum transaminases concentrations, and drug interactions. Some of these reactions have been of clinical significance. Presently, there are rare reports of gynecomastia, bradycardia, inhibition of acetylcholinesterase, headache, lethargy, diarrhea, and rash in patients receiving ranitidine. Antacids can produce either diarrhea or constipation and have been associated with low serum phosphorus concentrations, and metabolic alkalosis. Anticholinergics, especially in elderly or debilitated patients, can cause central nervous system disorders, intestinal atony, or urinary retention. Sucralfate may cause constipation, diarrhea, nausea, and headache. The investigational agents have their own side effect profiles. The adverse effects of anticholinergics make them unattractive therapeutic choices, and antacids and sucralfate have inconvenient dosing requirements compared with some equally efficacious alternatives. In addition, clinical experience with sucralfate in the United States is limited. The safety record of cimetidine is admirable. As clinical experience with ranitidine increases, currently unrecognized adverse effects may be reported. However, based on current data, ranitidine is as effective as cimetidine and is associated with a lower incidence of side effects.
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PMID:Problems associated with medical treatment of peptic ulcer disease. 609 62

Extracts of Sesbania drummondii administered to chickens by oral intubation are lethal within several days. Effects are dose-dependent; a dose of 1% of body weight is uniformly lethal in 5 days. Signs of poisoning include weakness, depression (CNS), anorexia, diarrhea, ruffled feathers, cold feet, and rapid loss of body weight. Microscopic examination indicates damage to kidney glomeruli and leakage of protein into the kidney tubules. Packed cell volume and plasma glucose concentrations show no difference between controls and treated chickens; however, creatine kinase is increased and plasma cholinesterase and total plasma protein values are severely depressed in poisoned birds. Neither a specific toxin nor a mechanism of action for toxicity has yet been identified.
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PMID:Determination of the oral toxicity of Sesbania drummondii seeds in chickens. 673 32

Dimethoate, an organophosphorus insecticide, was the suspected cause of toxicosis in a group of young cattle grazing on pasture that had been sprayed 6 weeks before the onset of clinical signs. Affected animals had primarily nicotinic signs, such as muscle twitching, stiffness, weakness and paralysis, though muscarinic signs, such as diarrhea, salivation and pollakiuria, were also observed. Whole blood acetylcholinesterase activity was depressed in 3 animals. The atypical clinical syndrome and poor response to treatment with atropine and other anticholinergics may have been due to coexistent hypomagnesemia.
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PMID:Suspected dimethoate toxicity in cattle. 673 94

28 cases of phallinic syndrome have been studied: 24 out of them were from amanita phalloides poisoning and 4 from amanita verna poisoning. After a lag phase lasting from 7 to 30 hours, symptomatology characterized by starting gastroenteric troubles as vomit, diarrhea, abdominal cramps, meteorism and pain following abdomen palpation. In one case the syndrome started with parasympathicomimetic crisis, probabily due to ingested amanita containing muscarinic type poison. Subsequent evolution of clinical picture included signs of hepatic and renal involvement. As far as laboratory diagnosis is concerned, high levels of serum aminotransferases were found and, less frequently, hyperbilirubinmia and high BUN levels occurred. In severe cases, in addition, lowered values for plasma prothrombine, fibrinogen and cholinesterase were found. Low therapeutic effect followed rehydration, equilibration of electrolytic unbalance and administration of thioctic acid, coagulants and so on. As a matter of fact 3 out or 28 patients, treated only with such therapy, died. On the contrary good therapeutic effect followed to peritoneal dialysis, in two cases coupled to exchange transfusion: 10 patients were treated in such a way and no one died but all of them quickly recovered. Forced diuresis also appeared greatly useful and practical in therapeutic treatment of phallinic syndrome: results compared favourably with those obtained by means of peritoneal dialysis. As a matter of fact 15 patients, 5 of them having ingested a great amount of amanita phalloides, were treated with forced diuresis and no one of them died. Finally, the need is stressed for a very quick therapeutic intervention (exchange transfusion; plasmapheresis; peritoneal dialysis; forced diuresis, and so on) in order to lower the plasma concentration of the toxins responsible for the phallinic syndrome. Only in such a way diffusion of toxins from blood to tissues is avoided.
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PMID:[Phallin syndrome. Reports on 28 cases]. 679 69


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