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Myocardial Receptors and Their Interaction with Cardiovascular Drugs

  • Chapter
PET for Drug Development and Evaluation

Part of the book series: Developments in Nuclear Medicine ((DNUM,volume 26))

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Abstract

Receptor abnormalities have been documented in myocardial samples obtained by endomyocardial biopsy or during surgery or autopsy. Positron Emission Tomography now allows to obtain noninvasively quantitative determination of regional receptor density and affinity in humans as well as innervation integrity and function. These measurements are based upon the synthesis of a radioligand, usually either a selective receptor antagonist or a false neurotransmitter labeled with a positron-emitting radioisotope. Mathematical compartmental models are fitted to activity vs.time curves obtained during saturation or displacement experiments in order to calculate the rate constants and the receptor density in meaningful regions-of-interest selected in the myocardium. Several receptor classes, adrenergic, muscarinic-cholinergic, peripheral-type benzodiazepine, have thus been characterized in humans. PET can help understand changes in cardiac innervation.

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Authors and Affiliations

  1. Service Hospitalier Frédéric Joliot, Département de Recherche Médicale, Commissariat à l’Energie Atomique, Orsay, France

    André Syrota MD, PhD & Pascal Merlet MD

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  1. André Syrota MD, PhD
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  2. Pascal Merlet MD
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  1. Hôpital Neuro-cardiologique, Lyon, France

    D. Comar

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Syrota, A., Merlet, P. (1995). Myocardial Receptors and Their Interaction with Cardiovascular Drugs. In: Comar, D. (eds) PET for Drug Development and Evaluation. Developments in Nuclear Medicine, vol 26. Springer, Dordrecht. https://doi.org/10.1007/978-94-011-0429-6_21

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  • DOI: https://doi.org/10.1007/978-94-011-0429-6_21

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