Modulation of forskolin-mediated adenylyl cyclase activation by constitutively active G(S)-coupled receptors

FEBS Letters
A E AlewijnseR Leurs

Abstract

In transfected CHO cells constitutively active histamine H2 receptors not only increase the basal cAMP level, but also enhance forskolin-induced cAMP production. The increased forskolin response was inhibited by inverse H2 agonists with potencies similar to those determined at basal levels. The modulation of the forskolin response was also observed after H2 receptor expression in HEK-293 and Sf9 cells or TSH receptor expression in COS-7 cells. The enhancement of forskolin-induced cAMP production seems to be a general characteristic of constitutively active G(S)-coupled receptors and can be very useful to study inverse agonism at wild-type receptors.

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Citations

Jan 5, 2001·British Journal of Pharmacology·M S Rodriguez-PenaR Leurs
Mar 22, 2002·British Journal of Pharmacology·Kurt A Krobert, Finn Olav Levy
Oct 30, 2007·The Journal of Pharmacology and Experimental Therapeutics·Sergey RyzhovIgor Feoktistov
Feb 18, 2011·British Journal of Pharmacology·J Daniel HothersallJames R Baker
Jul 15, 2004·Pigment Cell Research·Jesús Sánchez-MásCelia Jiménez-Cervantes
Feb 20, 2016·Environmental Health Perspectives·Mathilde MunierPatrice Rodien
Feb 21, 2003·The Journal of Biological Chemistry·Donald VanLeeuwenRobert G MacKenzie
Jan 6, 2001·Molecular Endocrinology·W A NijenhuisR A Adan
Apr 12, 2003·Journal of Receptor and Signal Transduction Research·Timothy A EsbenshadeArthur A Hancock
May 21, 2008·The Journal of Immunology : Official Journal of the American Association of Immunologists·Sergey RyzhovIgor Feoktistov
Jun 29, 2018·Molecular Pharmacology·Monica Soto-VelasquezVal J Watts

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