Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the beta2-adrenoceptor

Article Abstract:

Model studies of inverse agonist effects in transgenic mice with myocardial overexpression of beta2-adrenoceptor in the active conformation confirm the existence of inverse agonists. Beta-2-adrenoceptor ligand ICI-118,551 acts as an inverse agonist having an affinity for inactive conformation. ICI-118,551 inhibits baseline left atrial tension. These results validate the two-state model of G-protein-coupled receptor activation.

Epinephrine, Adrenergic receptors

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Painful connection for ATP

Article Abstract:

A study of role of adenosine 5'-triphosphate (ATP) in generating pain signals reveals that ATP may be initiating a nociceptive signal, acting as a neurotransmitter and purinoceptors for the generation of pain. A model for explaining the generation of pain by ATP in a human blister-base model is discussed. This research may indicate that pain relief through selective therapeutic agents is feasible.

Cytochemistry, Cell membranes, Plasma membranes, Adenosine triphosphate, ATP

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Inverse agonists exposed

Article Abstract:

Analysis of a transgenic mouse model with an overexpressed excitatory cardiac receptor provides evidence for the existence of inverse agonists. This analysis also validates the two-state model of G-protein-coupled receptor activation. This validation equips the model with pharmacological applications in the characterization and development of drugs.

Models

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