Partial agonist activity of carteolol on atypical beta-adrenoceptors in the guinea pig duodenum.

@article{Horinouchi2000PartialAA,
  title={Partial agonist activity of carteolol on atypical beta-adrenoceptors in the guinea pig duodenum.},
  author={Takahiro Horinouchi and Katsuo Koike},
  journal={European journal of pharmacology},
  year={2000},
  volume={403 1-2},
  pages={
          133-8
        }
}
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6 Citations

Agonistic activity of SR59230A at atypical beta-adrenoceptors in guinea pig gastric fundus and duodenum.

Partial agonistic activity of labetalol, the arylethanolamine, on beta 3-adrenoceptors in the guinea-pig gastric fundus.

The results indicate that labetalol, the arylethanolamine, acts as a partial agonist on beta3-adrenoceptors in the guinea-pig gastric fundus.

Functional properties of atypical β-adrenoceptors on the guinea pig duodenum

Further evidence that (+/-)-carteolol-induced relaxation is mediated by beta2-adrenoceptors but not by beta3-adrenoceptors in the guinea pig taenia caecum.

The results suggest that the relaxant effects of (+/-)-carteolol in the guinea pig taenia caecum are mediated by beta2-adrenoceptors but not by beta3- adrenOceptors.

Further characterization of β3-adrenoceptors in the guinea pig gastric fundus: stereoselectivity, β-adrenoceptor alkylation, and structure-activity relationship

Isomeric activity ratios for isomers of isoprenaline and noradrenaline were less than those obtained for activation of β1- and β2-adrenoceptors in the guinea pig atria and trachea, respectively.

β2-Adrenoceptor-mediated intrinsic sympathomimetic activity of carteolol: an in vivo study

The fact that the cardiovascular effects of carteolol were not attenuated by the β1-adrenoceptor blocker bisoprolol and, on the other, carteoolol significantly decreased lymphocyte β2-adRenoceptor density and function is in favour of the idea that the ISA of cartaolol is mediated byβ2- adrenoceptors.

References

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Characterization of atypical β-adrenoceptors in the guinea pig duodenum

A possible mechanism of action of a beta-adrenergic partial agonist (carteolol) in guinea pig taenia caecum.

Carteolol, 5-(3-tert-butylamino-2-hydroxy)propoxy-3, 4-dihydrocarbostyril hydrochloride was found to be a beta-adrenergic partial agonist in the taenia caecum of guinea pig. Concentration response…

Pharmacological Analysis of Atypical β-Adrenoceptors in the Guinea Pig Gastric Fundus Using the β3-Adrenoceptor Antagonist Bupranolol

Results clearly suggest that the existence of functional atypical β-adrenoceptors in the guinea pig gastric fundus and the relaxation of these agonists in this tissue are mediated via atypicals β- adrenOceptors.

Involvement of beta 3-adrenoceptor in the relaxation response in guinea pig taenia caecum.

The results suggest that isoprenaline-, noradrenaline- and adrenaline-induced relaxations of the guinea pig taenia caecum predominantly involve beta 2- and beta 3-adrenoceptors, whereas CGP 12177-induced relaxation is mediated solely through beta 3.

A trial for kinetic evaluation of the antagonistic potency of several beta-antagonists on presynaptic beta-adrenoceptors.

Carteolol has the highest pA2 and is a useful tool for clarifying whether or not presynaptic beta-adrenoceptors tonically function, and dose-dependently antagonized the isoproterenol-induced increases.

Possible mechanisms of beta-adrenoceptor-mediated relaxation induced by noradrenaline in guinea pig taenia caecum.

Relationship between intrinsic activity of beta-adrenoceptor agonist and amount of spare receptors in guinea pig taenia caecum.

The results suggest that there are spare receptors for isoprenaline, but few for desisopropylprocaterol and carteolol in the smooth muscle.

Signal transduction pathway involved in beta 3-adrenoceptor-mediated relaxation in guinea pig taenia caecum.

The results suggest that the production of cyclic AMP contributes to the beta 3-adrenoceptor (or atypical beta-adRenoceptor)-mediated relaxation of the guinea pig taenia caecum.

Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes.

Because arotinolol is only a very weak and partial agonist on the beta3-receptors, direct stimulation of thermogenesis in brown adipose tissue is unlikely to be sufficient to cause significant weight loss.

Evaluation of partial β‐adrenoceptor agonist activity

A partial beta-adrenoceptor (beta-AR) agonist will exhibit opposite agonist and antagonist activity depending on the prevailing degree of adrenergic tone or the presence of a beta-AR agonist with…