BIOMAT Database Logo BIOMAT Database Logo

Effects of cyclic AMP- and cyclic GMP- phosphodiesterase inhibitors on immunological release of histamine and on lung contraction. 1981

N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl

1 Cyclic adenosine 3',5'-monophosphate (cyclic AMP)- and cyclic guanosine 3',5'-monophosphate (cyclic GMP)-phosphodiesterase activities from rat lung were selectively inhibited by ZK 62711 and M & B 22948, respectively. Theophylline and papaverine inhibited both activities. 2 Rat lung strips contracted by carbachol were relaxed by 4-(3-cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone (ZK 26711, EC25 = 7 x 10(-8)M) and 2-O-propoxyphenyl-8-azapurin-6-one (M & B 22948, EC25 = 5 x 10(-7)M) indicating relaxant properties of both cyclic AMP and cyclic GMP. 3 The antigen-induced histamine release from human basophils was inhibited by ZK 62711 (IC25 = 8 x 10(-7)M), whereas M & B 22948 had no effect. On the contrary, the release from rat mast cells was inhibited by M & B 22948 (IC25 = 10(-6)M), while ZK 62711 had no effect. 4 These data show an inhibitory effect of cyclic AMP on histamine release to be involved with basophils, whereas cyclic GMP is predominantly involved with mast cells. Is is suggested that the antianaphylactic properties of cyclic nucleotide phosphodiesterase inhibitors are mainly linked to the increase of cyclic GMP.

UI MeSH Term Description Entries
D008168 Lung Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood. Lungs
D008297 Male Males
D010208 Papaverine An alkaloid found in opium but not closely related to the other opium alkaloids in its structure or pharmacological actions. It is a direct-acting smooth muscle relaxant used in the treatment of impotence and as a vasodilator, especially for cerebral vasodilation. The mechanism of its pharmacological actions is not clear, but it apparently can inhibit phosphodiesterases and it may have direct actions on calcium channels. Cerespan,Papaverine Hydrochloride,Pavabid,Pavatym,Hydrochloride, Papaverine
D011688 Purinones Oxopurines
D011760 Pyrrolidinones A group of compounds that are derivatives of oxo-pyrrolidines. A member of this group is 2-oxo pyrrolidine, which is an intermediate in the manufacture of polyvinylpyrrolidone. (From Merck Index, 11th ed) Pyrrolidinone,Pyrrolidone,Pyrrolidones
D003517 Cyclopentanes A group of alicyclic hydrocarbons with the general formula R-C5H9. Cyclopentadiene,Cyclopentadienes,Cyclopentene,Cyclopentenes,Cyclopentane
D004205 Cromolyn Sodium A chromone complex that acts by inhibiting the release of chemical mediators from sensitized MAST CELLS. It is used in the prophylactic treatment of both allergic and exercise-induced asthma, but does not affect an established asthmatic attack. Disodium Cromoglycate,Sodium Cromoglycate,Aarane,Bicromat Spray,Cromoglicic Acid,Cromoglycate,Cromoglycic Acid,Cromolyn,FPL-670,Intal,Lomudal,Nalcrom,Nasalcrom,Opticrom,Vicrom,Acid, Cromoglicic,Acid, Cromoglycic,Cromoglycate, Disodium,Cromoglycate, Sodium,FPL 670,FPL670
D006152 Cyclic GMP Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed) Guanosine Cyclic 3',5'-Monophosphate,Guanosine Cyclic 3,5 Monophosphate,Guanosine Cyclic Monophosphate,Guanosine Cyclic-3',5'-Monophosphate,3',5'-Monophosphate, Guanosine Cyclic,Cyclic 3',5'-Monophosphate, Guanosine,Cyclic Monophosphate, Guanosine,Cyclic-3',5'-Monophosphate, Guanosine,GMP, Cyclic,Guanosine Cyclic 3',5' Monophosphate,Monophosphate, Guanosine Cyclic
D006636 Histamine Release The secretion of histamine from mast cell and basophil granules by exocytosis. This can be initiated by a number of factors, all of which involve binding of IgE, cross-linked by antigen, to the mast cell or basophil's Fc receptors. Once released, histamine binds to a number of different target cell receptors and exerts a wide variety of effects. Histamine Liberation,Histamine Liberations,Histamine Releases
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man

Related Publications

N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Effects of phosphodiesterase inhibitors, imidazole and phosphate on cyclic CMP phosphodiesterase are different from those on cyclic AMP and cyclic GMP phosphodiesterases.
December 1978, Journal of cyclic nucleotide research,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Complex effects of inhibitors on cyclic GMP-stimulated cyclic nucleotide phosphodiesterase.
December 1983, The Journal of biological chemistry,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Inhibition of human lung cyclic GMP and cyclic AMP phosphodiesterases by certain nucleosides, nucleotides, and pharmacological phosphodiesterase inhibitors.
April 1979, Biochemical pharmacology,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Implication of cyclic AMP in the positive inotropic effects of cyclic GMP-inhibited cyclic AMP phosphodiesterase inhibitors on guinea pig isolated left atria.
March 1990, Journal of cardiovascular pharmacology,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Cyclic AMP phosphodiesterase and cyclic GMP phosphodiesterase activities of rat mammary tissue.
May 1984, The Biochemical journal,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Differential effects of various phosphodiesterase inhibitors, pyrimidine and purine compounds, and inorganic phosphates on cyclic CMP, cyclic AMP and cyclic GMP phosphodiesterases.
January 1982, Biochemical pharmacology,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Effects of phosphodiesterase inhibitors on cyclic AMP levels and on lipolysis.
December 1971, Annals of the New York Academy of Sciences,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Cyclic AMP-phosphodiesterase activity and histamine release in cord blood leukocyte preparations.
January 1985, Acta dermato-venereologica. Supplementum,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Effects of derivatives of cyclic amp and cyclic gmp on contraction force of cat papillary muscles.
March 1976, European journal of pharmacology,
N Frossard, and Y Landry, and G Pauli, and M Ruckstuhl
Cyclic AMP and cyclic GMP phosphodiesterase activities in Hodgkin's disease lymphocytes.
January 1987, International journal of immunopharmacology,
Copied contents to your clipboard!