Abstract
Ethylenediamine (EDA) released [3H]‐γ‐aminobutyric acid ([3H]‐GABA) in a dose‐dependent manner from the isolated preloaded ileum of the guinea‐pig maintained in Krebs‐bicarbonate solution (pH 7.4, 37°C), in the presence of β‐alanine and amino‐oxyacetic acid (AOAA) to prevent GABA uptake into glial cells and catabolism. This release was reversibly prevented by 3‐mercaptopropionic acid (3‐MPA), also in a dose‐dependent manner. In the isolated ileal preparations of the guinea‐pig maintained in Krebs‐bicarbonate solution, EDA induced a dose‐dependent transient, cholinergic contractile response (GABAA‐receptor‐mediated effect), followed by an ‘after‐relaxation’ (GABAB‐receptor‐mediated effect). EDA also induced a transient contraction superimposed on repetitive twitch responses to electrical transmural stimulation of the cholinergic neurones, followed by a depression of the twitch contractions. This GABAA‐receptor‐mediated contraction was antagonized by bicuculline methochloride and picrotoxinin, whilst the GABAB‐receptor‐mediated ‘after‐relaxation’, and depression of cholinergic twitch contractions, was susceptible to antagonism by δ‐aminovaleric acid. The pA2 value for bicuculline methochloride antagonism of EDA was estimated to be 5.8, identical with that for GABA. 3‐Mercaptopropionic acid also prevented these pharmacological actions induced by EDA without affecting responses to GABA, 3‐aminopropranesulphonic acid, muscimol, baclofen or the twitch responses to transmural stimulation. It is concluded that EDA releases both [3H]‐GABA and endogenous GABA in the guinea‐pig ileum, thus providing further evidence that GABA is a transmitter in the enteric nervous system.
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Dates
Type | When |
---|---|
Created | 13 years, 1 month ago (July 20, 2012, 4:56 a.m.) |
Deposited | 1 year, 10 months ago (Oct. 19, 2023, 11:13 p.m.) |
Indexed | 1 year, 10 months ago (Oct. 24, 2023, 3:57 a.m.) |
Issued | 41 years ago (Sept. 1, 1984) |
Published | 41 years ago (Sept. 1, 1984) |
Published Online | 13 years, 1 month ago (July 19, 2012) |
Published Print | 41 years ago (Sept. 1, 1984) |
@article{Kerr_1984, title={Evidence that ethylenediamine acts in the isolated ileum of the guinea‐pig by releasing endogenous GABA}, volume={83}, ISSN={1476-5381}, url={http://dx.doi.org/10.1111/j.1476-5381.1984.tb10132.x}, DOI={10.1111/j.1476-5381.1984.tb10132.x}, number={1}, journal={British Journal of Pharmacology}, publisher={Wiley}, author={Kerr, D.I.B. and Ong, Jennifer}, year={1984}, month=sep, pages={169–177} }