Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Young adult mice were inoculated in the hind limb with rabies virus or Sindbis virus. Rabies 1820B virus antigen was detected in leg sections by immuno-fluorescence at 1 h post-inoculation at sites comparable in form and distribution to cholinesterase-positive sites, which represent motor end-plates (MEPs). Sites which were rabies virus antigen-positive by immunofluorescence were also cholinesterase- positive on double-stained slides. Rabies CVS virus detected by autoradiography was similarly distributed at 6 h post-inoculation. Uptake of rabies virus at motor nerve endings was confirmed by the detection of rabies antigen by immunofluorescence in ventral horn cells in the spinal cord at 20 h post-inoculation before involvement of dorsal root ganglia. Rabies virus antigen could not be detected at MEPs if the virus had been inactivated by beta propiolactone or mixed with antibody prior to injection or if the sciatic nerve had been cut 7 days earlier, similarly treated groups of mice survived for the observation period of 6 weeks. Rabies virus antigen was found at MEPs in mice given antibody 24 h before virus injection, but virus antigen was not found in the spinal cord, and mice similarly treated survived. Sindbis virus strain Ar86, which like rabies virus is neurotropic in adult mice, was also found at MEPs and in peripheral nerves by autoradiography at 6 h post-inoculation. In contrast to results with rabies virus-infected mice, stimulation of the sciatic nerve for the first hour post-inoculation prevented mortality. Sindbis virus strain Ar339, which is not neurotropic in adult mice, could not be detected at MEP's by immunofluorescence or autoradiography and mice injected with virus survived. The results presented here suggest that rabies virus and perhaps other neurotropic viruses can use the motor axon terminal at the neuromuscular junction as a site of entry into the nervous system.
J Gen Virol 1981 Oct
PMID:Entry of rabies virus into the peripheral nerves of mice. 703 Nov 82

1. The effects of acute oral administration of carbaryl (10-80 mg/kg), a carbamate insecticide, on some experimental models for detecting dopaminergic activity were examined in rats. Also, serum biochemical variables following carbaryl treatments were determined. 2. Carbaryl (20 and 40 mg/kg) significantly increased the number of apomorphine-induced yawns and at dose of 80 mg/kg it prolonged the duration time of haloperidol-induced catalepsy. Pretreatment with carbaryl failed to affect apomorphine-induced stereotypes. 3. Carbaryl significantly reduced blood cholinesterase activity and elevated blood glucose levels and SGOT and SGPT activities. 4. These results indicate that low oral doses of carbaryl can cause behavioral and toxicological effects in rats.
Gen Pharmacol 1994 Oct
PMID:Effects of carbaryl on some dopaminergic behaviors in rats. 787 55

1. Habituation was regarded as a difference between exploratory activity measured first (session 1) and that measured second (session 2) in a novel environment. 2. Scopolamine (1.0 mg/kg) significantly increased the horizontal activity in sessions 1 and 2 when administered prior to session 1, resulting in the impairment of habituation. 3. Haloperidol (0.2 mg/kg) inhibited scopolamine-induced hypermotility in session 1, but it did not inhibit the scopolamine-induced impairment of habituation in session 2. 4. The direct cholinergic agonist oxotremorine (0.03 mg/kg), unlike the cholinesterase inhibitor physostigmine, significantly inhibited the scopolamine-induced impairment of habituation in the horizontal and vertical activities. 5. These results suggest that the direct stimulation of cholinergic receptors is more effective for scopolamine-induced amnesia than the indirect stimulation of cholinergic receptors by cholinesterase inhibitors in the habituation task.
Gen Pharmacol 1994 May
PMID:Characterization of the effects of scopolamine on the habituation of exploratory activity: differential effects of oxotremorine and physostigmine. 792 87

1. The negative chronotropic effects of acetylcholine and carbachol on isolated rat right atria were examined at 0, 4, 8, and 16 weeks after birth. 2. Acetylcholine produced negative chronotropic responses at all ages and completely abolished spontaneous beating at its maximum effective concentration. 3. The sensitivity to acetylcholine, expressed in terms of ED50 values, was higher at 0 and 4 weeks than at 8 and 16 weeks, ED50 values (microM) at 0, 4, 8 and 16 weeks being 9.5 +/- 1.8 (n = 12), 13.2 +/- 3.4 (n = 11), 59.3 +/- 10.9 (n = 14) and 51.5 +/- 17.5 (n = 5), respectively. 4. Neostigmine produced a leftward shift of the concentration-response curve for acetylcholine both at 4 and 8 weeks after birth. The shift was larger at 8 weeks and no difference in sensitivity to acetylcholine was observed between the two ages in the presence of neostigmine. 5. Further, no developmental changes were observed in the sensitivity to carbachol, which is not hydrolyzed by cholinesterase. 6. We concluded that the chronotropic sensitivity to acetylcholine of rat atria decreases post-natally during the period between 4 and 8 weeks after birth due to increase in cholinesterase activity.
Gen Pharmacol 1994 Jan
PMID:Post-natal decrease in chronotropic sensitivity to acetylcholine in rat heart. 802 2

The distribution of cholinesterase (ChE) activity was demonstrated in the hypothalamo-hypophyseal system of Heteropneustes fossilis using acetylthiocholine iodide as the substrate. Perikarya of neurons in nucleus lateralis tuberis and the periventricular region of the infundibular recess showed moderate to strong enzyme activity. In the midventral floor of the infundibular recess, the ependymal layer contained ChE-positive neurons, some of which contacted the ventricle. From these neurons, fine beaded axonal processes were seen to run across the fibrous layer close to ChE-positive capillaries. The blood vessels and capillaries in the external palisade layer also showed intense enzyme activity. The distributional pattern of ChE strongly suggests homology of the region with the median eminence of tetrapods. In the pituitary, the neurohypophysis was generally free of enzyme activity except for some displaced neurons, pituicytes, and capillaries. The hypophyseal blood vessels and capillaries showed strong enzyme activity which varied regionally.
Gen Comp Endocrinol 1994 Jan
PMID:Histochemical distribution of cholinesterase activity in the hypothalamo-hypophyseal system of the catfish, Heteropneustes fossilis. 813 9

1. The present study was designed to examine the effects of intracerebroventricular injection of several cholinergic drugs on the impairment of spontaneous alternation performance induced by the M1-selective muscarinic receptor antagonist pirenzepine. 2. Pirenzepine (3 and 10 micrograms) significantly reduced spontaneous alteration performance related to working memory without producing any marked increase in total arm entries, which are considered to reflect locomotor activity. 3. Physostigmine (3.47 micrograms), a cholinesterase inhibitor, and McN-A-343 (20 micrograms), and M1-selective muscarinic receptor agonist, significantly improved the pirenzepine (3 micrograms)-induced impairment of spontaneous alternation performance, although oxotremorine (0.68 microgram), a nonselective muscarinic receptor agonist, showed a tendency to reverse the pirenzepine (3 micrograms)-induced impairment. 4. These findings suggest that the blockade of muscarinic M1 but not M2 receptors results in the impairment of spontaneous alternation performance associated with working memory.
Gen Pharmacol 1995 Nov
PMID:Cholinergic receptor agonists inhibit pirenzepine-induced dysfunction of spontaneous alternation performance in the mouse. 869 Feb 40

The neurons of the caudal neurosecretory system of teleosts contain, in addition to urotensin I and urotensin II, a high concentration of acetylcholine (T. Ichikawa, 1978, Gen. Comp. Endocrinol. 35, 226-233). The isolated urophysis (and attached terminal spinal cord region) of the rainbow trout Oncorhynchus mykiss was incubated with [3H]choline (0.2 MBq/ml) for 45 min at 22 degrees in the presence of the cholinesterase inhibitor, physostigmine. Unreacted choline was removed by perifusion with fish Ringer solution. Incorporation of radioactivity into newly synthesized [3H]acetylcholine was 4.9 +/- 2.1 x 10(5) Bq/g wet tissue wt. When incubations were carried out in the presence of hemicholinium-3, an inhibitor of high-affinity choline uptake, or when physostigmine was omitted from the incubation buffer and/or when [3H]inulin was substituted for [3H]choline, the incorporation of radioactivity was greatly reduced (< 0.5 x 10(5) Bq/g). The release of [3H]acetylcholine from the preparation increased to 338 +/- 59% of basal (P < 0.05) when the concentration of K+ in the perifusion buffer was raised to 41 mM, but neither urotensin I (10(-7) M) nor urotensin II (10(-6) M) had a significant effect on release. The data indicate that the trout caudal neurosecretory system possesses a high-affinity uptake system for choline and that newly synthesized acetylcholine is released in response to a depolarizing stimulus.
Gen Comp Endocrinol 1996 Jul
PMID:Synthesis and release of acetylcholine by the isolated perifused trout caudal neurosecretory system. 881 28

1. A differential inhibition assay was developed for the quantitative determination of cholinesterase isoenzymes acetylcholinesterase (AChE; EC 3.1.1.7), cholinesterase (BChE; EC 3.1.1.8), and atypical cholinesterase in small samples of left ventricular porcine heart muscle. 2. The assay is based on kinetic analysis of irreversible cholinesterase inhibition by the organophosphorus compound N,N'-di-isopropylphosphorodiamidic fluoride (mipafox). With acetylthiocholine (ASCh) as substrate (1.25 mM), hydrolytic activities (A) of cholinesterase isoenzymes were determined after preincubation (60 min, 25 degrees C) of heart muscle samples with either saline (total activity, A tau), 7 microM mipafox (AM1), or 0.8 mM mipafox (AM2): (BChE) = A tau-AM1, (AChE) = AM1-AM2, (Atypical ChE) = AM2. 3. The mipafox differential inhibition assay was used to determine the substrate hydrolysis patterns of myocardial cholinesterases with ASCh, acetyl-beta-methylthiocholine (A beta MSCh), propionylthiocholine (PSCh), and butyrylthiocholine (BSCh). The substrate specificities of myocardial AChE and BChE resemble those of erythrocyte AChE and serum BChE, respectively. Michaelis constants KM with ASCh were determined to be 0.15 mM for AChE and 1.4 mM for BChE. 4. Atypical cholinesterase, in respect to both substrate specificity and inhibition kinetics, differs from cholinesterase activities of vertebrate tissue and, up to now, could be identified exclusively in heart muscle. The enzyme's Michaelis constant with ASCh was determined to be 4.0 mM. 5. The reversible inhibitory effects of physostigmine (eserine) and quinidine on heart muscle cholinesterases were investigated using the differential inhibition assay. With all three isoenzymes, the inhibition kinetics of both substances were strictly competitive. The physostigmine inhibition of AChE was most pronounced (Ki = 0.22 microM). Quinidine most potently inhibited myocardial BChE (Ki = 35 microM).
Gen Pharmacol 1997 Apr
PMID:Mipafox differential inhibition assay for heart muscle cholinesterases: substrate specificity and inhibition of three isoenzymes by physostigmine and quinidine. 914 26

1. The cholinesterases play an important role in the innervation of organs. The ratio of solubilized to membrane-bound cholinesterase and the quantitative distributions of acetylcholinesterase and butyrylcholinesterase were measured in different segments of the gut of carp (Cyprinus carpio) connected with different types of nerve-muscle synapses in different parts of the alimentary tract. 2. The inhibition of acetylcholinesterase (EC 3.1.1.7.) by the herbicide paraquat and the insecticide metidathion was measured in different parts of the gut of carp. 3. Metidathion and paraquat significantly decreased the activity of acetylcholinesterase in different segments of the alimentary tract of common carp, in a concentration-dependent manner.
Gen Pharmacol 1997 Jul
PMID:Quantitative distributions of different cholinesterases and inhibition of acetylcholinesterase by metidathion and paraquat in alimentary canal of common carp. 919 93

1. The effect of amitriptyline on human serum butyrylcholinesterase (acylcholine acylhydrolase E.C.3.1.1.8) has been investigated. From the Lineweaver-Burk plot and the plot of v versus amitriptyline concentration, it was concluded that amitriptyline inhibition is partially competitive, and the kinetic parameters have been calculated as Ks = 0.11 mM, alpha = 1425 and Ki = 0.01 mM. 2. Because amitriptyline is a partial competitive inhibitor of butyrylcholinesterase, acquired deficiency may be seen in patients treated with amitriptyline and may cause complications in operations.
Gen Pharmacol 1997 Nov
PMID:Amitriptyline: a potent inhibitor of butyrylcholinesterase from human serum. 934 35


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