β1- and β3-adrenoceptor mediated smooth muscle relaxation in hypothyroid rat ileum

Katherine J. Brown, Roger J. Summers

Research output: Contribution to journalArticleResearchpeer-review

Abstract

The effect of hypothyroidism on gastrointestinal β1- and β3-adrenoceptor function and expression was examined in rat ileal smooth muscle preparations. (-)-Isoprenaline and the selective β3 agonist disodium (R,R)-5-[2-[[2-3-chlorophenyl)-2-hydroxyethyl]-amino]propyl]-1,3- benzodioxole-2,2-dicarboxylate (CL 316234) relaxed both control and hypothyroid tissues in a dose-dependent manner. Responses to isoprenaline were reduced in tissues from hypothyroid rats, as was the shift produced with the β3-adrenoceptor antagonist, 3-(2-ethylphenoxy)-1-[(1S)-1,2,3,4-tetrahydronaphth-1-ylamino]-(2S)-2- propanol oxalate (SR 59230A). No change was seen in responses to CL 316243. Experiments with a selective β1-adrenoceptor antagonist produced results suggesting that isoprenaline did not act at this receptor. Messenger RNA levels for both β1- and β2-adrenoceptors were not affected by hypothyroidism. These results show that, unlike in adipose tissues, ileal β1- and β3-adrenoceptors are not directly regulated by thyroid hormone and that β3-adrenoceptor coupling to the relaxation response is reduced in a rat model of hypothyroidism.

Original languageEnglish
Pages (from-to)257-263
Number of pages7
JournalEuropean Journal of Pharmacology
Volume415
Issue number2-3
DOIs
Publication statusPublished - 16 Mar 2001

Keywords

  • β-Adrenoceptors
  • Hypothyroidism
  • Messenger RNA
  • Relaxation
  • Smooth muscle, Ileal

Cite this

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abstract = "The effect of hypothyroidism on gastrointestinal β1- and β3-adrenoceptor function and expression was examined in rat ileal smooth muscle preparations. (-)-Isoprenaline and the selective β3 agonist disodium (R,R)-5-[2-[[2-3-chlorophenyl)-2-hydroxyethyl]-amino]propyl]-1,3- benzodioxole-2,2-dicarboxylate (CL 316234) relaxed both control and hypothyroid tissues in a dose-dependent manner. Responses to isoprenaline were reduced in tissues from hypothyroid rats, as was the shift produced with the β3-adrenoceptor antagonist, 3-(2-ethylphenoxy)-1-[(1S)-1,2,3,4-tetrahydronaphth-1-ylamino]-(2S)-2- propanol oxalate (SR 59230A). No change was seen in responses to CL 316243. Experiments with a selective β1-adrenoceptor antagonist produced results suggesting that isoprenaline did not act at this receptor. Messenger RNA levels for both β1- and β2-adrenoceptors were not affected by hypothyroidism. These results show that, unlike in adipose tissues, ileal β1- and β3-adrenoceptors are not directly regulated by thyroid hormone and that β3-adrenoceptor coupling to the relaxation response is reduced in a rat model of hypothyroidism.",
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β1- and β3-adrenoceptor mediated smooth muscle relaxation in hypothyroid rat ileum. / Brown, Katherine J.; Summers, Roger J.

In: European Journal of Pharmacology, Vol. 415, No. 2-3, 16.03.2001, p. 257-263.

Research output: Contribution to journalArticleResearchpeer-review

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