Literature DB >> 7679027

Levamisole-activated single-channel currents from muscle of the nematode parasite Ascaris suum.

S J Robertson1, R J Martin.   

Abstract

1. The patch-clamp technique was used to examine levamisole-activated channels in muscle vesicles from Ascaris suum. Cell-attached and isolated inside-out patches were used. 2. Levamisole (1-90 microM), applied to the extracellular surface, activated channels which had apparent mean open-times in the range 0.80-2.85 ms and linear I/V relationships with conductances in the range 19-46 pS. Ion-replacement experiments showed the channels to be cation selective. 3. The kinetics of the channels were analysed. Generally open- and closed-time distributions were best fitted by two, and three exponentials respectively, indicating the presence of at least two open states and at least three closed states. The distributions of burst-times were best-fitted by two exponentials. 4. Channel open- and burst-times were voltage-sensitive: at low levamisole concentrations (1-10 microM), they increased with hyperpolarization. At higher concentrations of levamisole (30 microM and 90 microM) flickering channel-block was observed at hyperpolarized potentials. Using a simple channel-block model, values for the blocking dissociation constant, KB were determined as 123 microM at -50 mV, 46 microM at -75 mV and 9.4 microM at -100 mV. 5. At the higher concentration of levamisole (30 microM and 90 microM) long closed-times separating 'clusters' of bursts were observed, at both hyperpolarized and depolarized membrane potentials and this was interpreted as desensitization.

Entities:  

Mesh:

Substances:

Year:  1993        PMID: 7679027      PMCID: PMC1907687          DOI: 10.1111/j.1476-5381.1993.tb13458.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  17 in total

1.  Chemotherapy of intestinal helminthiasis.

Authors:  O D Standen
Journal:  Prog Drug Res       Date:  1975

2.  Local anaesthetics transiently block currents through single acetylcholine-receptor channels.

Authors:  E Neher; J H Steinbach
Journal:  J Physiol       Date:  1978-04       Impact factor: 5.182

3.  The mode of action of four anthelmintics.

Authors:  G C Coles; J M East; S M Jenkins
Journal:  Experientia       Date:  1974-11-15

4.  On the stochastic properties of bursts of single ion channel openings and of clusters of bursts.

Authors:  D Colquhoun; A G Hawkes
Journal:  Philos Trans R Soc Lond B Biol Sci       Date:  1982-12-24       Impact factor: 6.237

5.  The charge carried by single-channel currents of rat cultured muscle cells in the presence of local anaesthetics.

Authors:  E Neher
Journal:  J Physiol       Date:  1983-06       Impact factor: 5.182

6.  Pharmacological characteristics of cholinoreception in somatic muscles of the nematode, Ascaris suum.

Authors:  E K Rozhkova; T A Malyutina; B A Shishov
Journal:  Gen Pharmacol       Date:  1980

7.  Drug blockade of open end-plate channels.

Authors:  P R Adams
Journal:  J Physiol       Date:  1976-09       Impact factor: 5.182

8.  The pharmacology of the cholinoceptor in muscle preparations of Ascaris lumbricoides var. suum.

Authors:  I L Natoff
Journal:  Br J Pharmacol       Date:  1969-09       Impact factor: 8.739

9.  Electrophysiological effects of piperazine and diethylcarbamazine on Ascaris suum somatic muscle.

Authors:  R J Martin
Journal:  Br J Pharmacol       Date:  1982-10       Impact factor: 8.739

10.  The pharmacology of cholinoceptors on the somatic muscle cells of the parasitic nematode Ascaris suum.

Authors:  L Colquhoun; L Holden-Dye; R J Walker
Journal:  J Exp Biol       Date:  1991-07       Impact factor: 3.312

View more
  18 in total

1.  One GABA and two acetylcholine receptors function at the C. elegans neuromuscular junction.

Authors:  J E Richmond; E M Jorgensen
Journal:  Nat Neurosci       Date:  1999-09       Impact factor: 24.884

2.  Caenorhabditis elegans levamisole resistance genes lev-1, unc-29, and unc-38 encode functional nicotinic acetylcholine receptor subunits.

Authors:  J T Fleming; M D Squire; T M Barnes; C Tornoe; K Matsuda; J Ahnn; A Fire; J E Sulston; E A Barnard; D B Sattelle; J A Lewis
Journal:  J Neurosci       Date:  1997-08-01       Impact factor: 6.167

3.  TOMOCOMD-CARDD, a novel approach for computer-aided 'rational' drug design: I. Theoretical and experimental assessment of a promising method for computational screening and in silico design of new anthelmintic compounds.

Authors:  Yovani Marrero-Ponce; Juan A Castillo-Garit; Ervelio Olazabal; Hector S Serrano; Alcidez Morales; Nilo Castañedo; Froylán Ibarra-Velarde; Alma Huesca-Guillen; Elisa Jorge; Arletys del Valle; Francisco Torrens; Eduardo A Castro
Journal:  J Comput Aided Mol Des       Date:  2004-10       Impact factor: 3.686

4.  Eight genes are required for functional reconstitution of the Caenorhabditis elegans levamisole-sensitive acetylcholine receptor.

Authors:  Thomas Boulin; Marc Gielen; Janet E Richmond; Daniel C Williams; Pierre Paoletti; Jean-Louis Bessereau
Journal:  Proc Natl Acad Sci U S A       Date:  2008-11-19       Impact factor: 11.205

5.  Functional genomics in Brugia malayi reveal diverse muscle nAChRs and differences between cholinergic anthelmintics.

Authors:  Saurabh Verma; Sudhanva Srinivas Kashyap; Alan Patrick Robertson; Richard John Martin
Journal:  Proc Natl Acad Sci U S A       Date:  2017-05-09       Impact factor: 11.205

Review 6.  Levamisole receptors: a second awakening.

Authors:  Richard J Martin; Alan P Robertson; Samuel K Buxton; Robin N Beech; Claude L Charvet; Cédric Neveu
Journal:  Trends Parasitol       Date:  2012-05-17

Review 7.  Ion-channels on parasite muscle: pharmacology and physiology.

Authors:  Alan P Robertson; Richard J Martin
Journal:  Invert Neurosci       Date:  2007-11-13

8.  Activation and cooperative multi-ion block of single nicotinic-acetylcholine channel currents of Ascaris muscle by the tetrahydropyrimidine anthelmintic, morantel.

Authors:  A M Evans; R J Martin
Journal:  Br J Pharmacol       Date:  1996-07       Impact factor: 8.739

9.  Effects of the muscarinic agonist, 5-methylfurmethiodide, on contraction and electrophysiology of Ascaris suum muscle.

Authors:  Sasa M Trailovic; Saurabh Verma; Cheryl L Clark; Alan P Robertson; Richard J Martin
Journal:  Int J Parasitol       Date:  2007-12-08       Impact factor: 3.981

10.  Identification of an Ascaris G protein-coupled acetylcholine receptor with atypical muscarinic pharmacology.

Authors:  Michael J Kimber; Laura Sayegh; Fouad El-Shehabi; Chuanzhe Song; Mostafa Zamanian; Debra J Woods; Tim A Day; Paula Ribeiro
Journal:  Int J Parasitol       Date:  2009-03-25       Impact factor: 3.981

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.