-transparent.png){kind=logo}
8-(4-Chlorophenyl)thio-cyclic AMP (8-CPT-cAMP), extensively used as selective activator of cyclic AMP-dependent protein kinase, has been found to be a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA). Indeed, 8-CPT-cAMP (IC50 = 0.9 microM) inhibited PDE VA with a potency identical to that of zaprinast. 8-CPT-cAMP was also metabolized by PDE VA at a rate half that of cyclic GMP. The cyclic GMP-inhibited phosphodiesterase (PDE III) (IC50 = 24 microM) and the cyclic AMP-specific phosphodiesterase (PDE IV) (IC50 = 25 microM) were also inhibited by 8-CPT-cAMP. In contrast, most of the other cAMP-derivative studies showed little inhibition of any phosphodiesterase isoenzyme. These observations provide further reasons why the mechanism of the physiological effects of 8-CPT-cAMP should be interpreted with caution.
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
August 1985,
Methods and findings in experimental and clinical pharmacology,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
January 1991,
Agents and actions. Supplements,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
October 1993,
Neurochemical research,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
October 1995,
Molecular pharmacology,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
September 2014,
Metabolic brain disease,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
May 2000,
Immunopharmacology,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
May 1984,
The Biochemical journal,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
November 1993,
Journal of medicinal chemistry,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
June 1989,
Journal of autonomic pharmacology,
B J Connolly, and
P B Willits, and
B H Warrington, and
K J Murray
August 1990,
Biochemical pharmacology,
