Literature DB >> 2851353

ZAPA, (Z)-3-[(aminoiminomethyl)thio]-2-propenoic acid hydrochloride, a potent agonist at GABA-receptors on the Ascaris muscle cell.

L Holden-Dye1, R J Walker.   

Abstract

This study is the first report of a compound which is equal in efficacy to gamma-aminobutyric acid (GABA) at the nematode Ascaris muscle GABA-receptor. The GABA-receptor at the Ascaris muscle cell which mediates a membrane hyperpolarization and muscle relaxation has eluded classification. The structure-activity profile of this receptor is not typical of GABAA or GABAB-receptors. Here we report that the isothiouronium compound ZAPA is as potent as GABA at this receptor. This finding has important implications for the characterization of the Ascaris GABA-receptor and the design of novel anthelmintics.

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Year:  1988        PMID: 2851353      PMCID: PMC1854134          DOI: 10.1111/j.1476-5381.1988.tb16540.x

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


  6 in total

Review 1.  Pharmacological characterization of different types of GABA and glutamate receptors in vertebrates and invertebrates.

Authors:  A Nistri; A Constanti
Journal:  Prog Neurobiol       Date:  1979       Impact factor: 11.685

2.  The gamma-aminobutyric acid receptor of Ascaris as a target for anthelmintics.

Authors:  R J Martin
Journal:  Biochem Soc Trans       Date:  1987-02       Impact factor: 5.407

3.  Isothiouronium compounds as gamma-aminobutyric acid agonists.

Authors:  R D Allan; H W Dickenson; B P Hiern; G A Johnston; R Kazlauskas
Journal:  Br J Pharmacol       Date:  1986-06       Impact factor: 8.739

4.  The electrophysiology of the somatic muscle cells of Ascaris suum and Ascaridia galli.

Authors:  K T Wann
Journal:  Parasitology       Date:  1987-06       Impact factor: 3.234

5.  Inhibitory action of gamma-aminobutyric acid (GABA) on Ascaris muscle.

Authors:  J Del Castillo; W C De Mello; T Morales
Journal:  Experientia       Date:  1964-03-15

6.  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

  6 in total
  3 in total

1.  A molecular characterization of the agonist binding site of a nematode cys-loop GABA receptor.

Authors:  Mark D Kaji; Ariel Kwaka; Micah K Callanan; Humza Nusrat; Jean-Paul Desaulniers; Sean G Forrester
Journal:  Br J Pharmacol       Date:  2015-05-19       Impact factor: 8.739

2.  GABA receptors on the somatic muscle cells of the parasitic nematode, Ascaris suum: stereoselectivity indicates similarity to a GABAA-type agonist recognition site.

Authors:  L Holden-Dye; P Krogsgaard-Larsen; L Nielsen; R J Walker
Journal:  Br J Pharmacol       Date:  1989-11       Impact factor: 8.739

3.  Actions of acetylcholine and GABA on spontaneous contractions of the filariid, Dipetalonema viteae.

Authors:  D Christ; M Goebel; H J Saz
Journal:  Br J Pharmacol       Date:  1990-12       Impact factor: 8.739

  3 in total

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