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Compare endothelin ETA receptor desensitization and characterize the intracellular phosphorylation mechanisms governing heart-rate responses in rat versus guinea pig right atria.

October 1, 1998British Journal of PharmacologyOpen Access

Desensitization of ETA endothelin receptor‐mediated negative chronotropic response in right atria–species difference and intracellular mechanisms

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Compare endothelin ETA receptor desensitization and characterize the intracellular phosphorylation mechanisms governing heart-rate responses in rat versus guinea pig right atria.
Measured chronotropic responses in isolated rat and guinea-pig right atria challenged with repetitive endothelin-1 exposures in the presence of selective antagonists BQ788 and BQ123.
Tested receptor regulation using pharmacological modulators (staurosporine, PMA, okadaic acid, isoproterenol) and performed partial amino acid sequencing of intracellular loops 2 through 4 of ETA receptors.
Repeated endothelin-1 administration completely abolished the ETA-mediated negative chronotropic response in rat atria, whereas guinea-pig atria produced sustained, repeatable slowing responses without desensitization.
Conserved serine/threonine phosphorylation sites occurred across both species, but guinea-pig ETA receptors desensitized only under concurrent beta-adrenoceptor stimulation combined with phosphatase inhibition and protein kinase C activation.

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Implication

Experimental study reveals species-dependent desensitization of cardiac endothelin ETA receptors between rats and guinea pigs, indicating divergent phosphorylation environments regulate receptor...

Cite This Study

Ono et al. (1998) studied this question.

synapsesocial.com/papers/6a83ec996eaad3b729ee9142 https://doi.org/10.1038/sj.bjp.0702125

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Implication

Experimental study reveals species-dependent desensitization of cardiac endothelin ETA receptors between rats and guinea pigs, indicating divergent phosphorylation environments regulate receptor...

Desensitization of ETA endothelin receptor‐mediated negative chronotropic response in right atria–species difference and intracellular mechanisms

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Discussion

Implication

Cite This Study

Desensitization of ETA endothelin receptor‐mediated negative chronotropic response in right atria–species difference and intracellular mechanisms

Key Points

Discussion

Implication

Cite This Study

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