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1,4-Cyclohexanecarboxylates: Potent and Selective Inhibitors of Phosophodiesterase 4 for the Treatment of Asthma

artículo científico publicado el 12 de marzo de 1998

A Candida albicans cyclic nucleotide phosphodiesterase: cloning and expression in Saccharomyces cerevisiae and biochemical characterization of the recombinant enzyme

artículo científico publicado en 1994

A low-Km, rolipram-sensitive, cAMP-specific phosphodiesterase from human brain. Cloning and expression of cDNA, biochemical characterization of recombinant protein, and tissue distribution of mRNA

artículo científico publicado en 1993

Action of mediators on airway smooth muscle: functional antagonism as a mechanism for bronchodilator drugs

artículo científico publicado en 1988

Activation of cyclic AMP-dependent protein kinase during canine lower esophageal sphincter relaxation

scientific article published on 01 March 1990

Agonist-related differences in the relationship between cAMP content and protein kinase activity in canine trachealis

artículo científico publicado el 1 de junio de 1992

Antiasthmatic activity of the second-generation phosphodiesterase 4 (PDE4) inhibitor SB 207499 (Ariflo) in the guinea pig.

artículo científico publicado en 1998

Association between leukotriene B4-induced phospholipase D activation and degranulation of human neutrophils

artículo científico publicado en 1993

Association of the anti-inflammatory activity of phosphodiesterase 4 (PDE4) inhibitors with either inhibition of PDE4 catalytic activity or competition for [3H]rolipram binding

artículo científico publicado en 1996

Beta-adrenoceptors, cAMP and airway smooth muscle relaxation: challenges to the dogma

artículo científico publicado en 1994

Biochemical characteristics and cellular regulation of phosphodiesterase IV.

artículo científico publicado en 1993

Biochemical regulation of airway smooth muscle tone: current knowledge and therapeutic implications

artículo científico publicado en 1987

Biopharmaceutical therapeutics for asthma remodeling

artículo científico publicado en 2006

Characterization and selective inhibition of cyclic nucleotide phosphodiesterase isozymes in canine tracheal smooth muscle

artículo científico publicado en 1990

Characterization of two human cAMP‐specific phosphodiesterase subtypes expressed in baculovirus‐infected insect cells

artículo científico publicado el 1 de junio de 1995

Cloning and expression of cDNA for a human low-Km, rolipram-sensitive cyclic AMP phosphodiesterase

artículo científico publicado en 1990

Coexpression of human cAMP-specific phosphodiesterase activity and high affinity rolipram binding in yeast

artículo científico publicado el 25 de enero de 1992

Coming of age: anti-cytokine therapies

artículo científico publicado en 2002

Comparison of phosphodiesterase III, IV and dual III/IV inhibitors on bronchospasm and pulmonary eosinophil influx in guinea pigs

artículo científico publicado en 1994

Critical role of conserved histidine pairs HNXXH and HDXXH in recombinant human phosphodiesterase 4A

scientific article published on 01 July 1998

Cyclic GMP-dependent protein kinase activation in canine tracheal smooth muscle by methacholine and sodium nitroprusside

artículo científico publicado el 11 de diciembre de 1984

Cyclic GMP: a potential mediator of neurally- and drug-induced relaxation of opossum lower esophageal sphincter

artículo científico publicado en 1989

Cyclic nucleotide-dependent protein kinases in airway smooth muscle

artículo científico publicado el 10 de octubre de 1982

Cyclic nucleotide-dependent protein kinases in the lower esophageal sphincter

scientific article published on 01 December 1986

Cysteinyl leukotrienes in asthma: old mediators up to new tricks

artículo científico publicado en 1995

Differences in the ability of salbutamol to prevent and reverse LTC4-induced contractions of the guinea-pig isolated trachea: influence of l-serine borate

artículo científico publicado en 1986

Differential relaxant effects of isoproterenol on methacholine- versus leukotriene D4-induced contraction in the guinea-pig trachea

artículo científico publicado en 1984

Dissociation between myosin phosphorylation and shortening velocity in canine trachea

artículo científico publicado en 1990

Effect of reserpine pretreatment on mechanical responsiveness and [125I]Iodohydroxybenzylpindolol binding sites in the guinea-pig right atrium

artículo científico publicado el 1 de noviembre de 1982

Effect of selective phosphodiesterase type IV inhibitor, rolipram, on fluid and cellular phases of inflammatory response

artículo científico publicado el 1 de junio de 1993

Evaluation of human cytokine production and effects of pharmacological agents in a heterologous system in vivo

artículo científico publicado en 1996

Expression of human recombinant cAMP phosphodiesterase isozyme IV reverses growth arrest phenotypes in phosphodiesterase-deficient yeast

artículo científico publicado el 1 de febrero de 1991

Functional antagonism by salbutamol suggests differences in the relative efficacies and dissociation constants of the peptidoleukotrienes in guinea pig trachea.

artículo científico publicado en 1988

Functional antagonism in canine tracheal smooth muscle: inhibition by methacholine of the mechanical and biochemical responses to isoproterenol

artículo científico publicado el 1 de diciembre de 1983

Identification, characterization and functional role of phosphodiesterase isozymes in human airway smooth muscle

artículo científico publicado en 1993

Identification, characterization, and functional role of phosphodiesterase type IV in cerebral vessels: effects of selective phosphodiesterase inhibitors

scientific article published on 01 February 1997

Inactivation of recombinant monocyte cAMP-specific phosphodiesterase by cAMP analog, 8-[(4-bromo-2,3-dioxobutyl)thio]adenosine 3',5'-cyclic monophosphate

scientific article published on 01 February 1997

Influence of isoproterenol and phosphodiesterase inhibitors on platelet-activating factor biosynthesis in the human neutrophil

scientific article published on 01 July 1993

Inhibition by adenosine 3':5'-monophosphate of eicosanoid and platelet-activating factor biosynthesis in the mouse PT-18 mast cell

artículo científico publicado el 25 de abril de 1990

Inhibition of antigen-induced bronchoconstriction and eosinophil infiltration in the guinea pig by the cyclic AMP-specific phosphodiesterase inhibitor, rolipram.

artículo científico publicado en 1993

Inhibition of leukotriene D4-induced coronary vasoconstriction by leukotriene antagonists in the anesthetized dog

artículo científico publicado en 1987

Inhibitors of CoA-independent transacylase block the movement of arachidonate into 1-ether-linked phospholipids of human neutrophils

artículo científico publicado en 1995

Inhibitors of phosphodiesterase IV (PDE IV) increase acid secretion in rabbit isolated gastric glands: correlation between function and interaction with a high-affinity rolipram binding site

scientific article published on 01 June 1995

Inhibitory effect of methacholine on drug-induced relaxation, cyclic AMP accumulation, and cyclic AMP-dependent protein kinase activation in canine tracheal smooth muscle

artículo científico publicado en 1985

Is the guinea pig trachea a good in vitro model of human large and central airways? Comparison on leukotriene-, methacholine-, histamine- and antigen-induced contractions

artículo científico publicado en 1987

Lower esophageal sphincter relaxation is associated with increased cyclic nucleotide content

artículo científico publicado en 1986

Mapping the functional domains of human recombinant phosphodiesterase 4A: structural requirements for catalytic activity and rolipram binding.

artículo científico publicado en 1996

Mechanisms of adaptive supersensitivity: correlation of guinea pig atrial supersensitivity with modifications in adenylyl cyclase activity

artículo científico publicado en 1997

Methacholine sensitivity and cAMP protein kinase in tracheal smooth muscle

artículo científico publicado en 1986

Monoclonal antibodies as a strategy for pulmonary diseases

artículo científico publicado en 2001

Open partnering of integrated drug discovery: continuing evolution of the pharmaceutical model

artículo científico publicado el 15 de febrero de 2011

Ovarian effects of SK&F 86002-A2 in the rat: site of action

artículo científico publicado en 1988

PDE inhibitors--Second William Harvey Research Conference. Drugs with an expanding range of therapeutic uses. 1-3 December 1999, Nice, France

artículo científico publicado en 2000

Persistent airway eosinophilia after leukotriene (LT) D4 administration in the guinea pig: modulation by the LTD4 receptor antagonist, pranlukast, or an interleukin-5 monoclonal antibody

artículo científico publicado en 1996

Pharmacologic profile of SK&F 104353, a novel, highly potent and selective peptidoleukotriene antagonist

artículo científico publicado en 1987

Pharmacologic profile of SK&F 104353: a novel, potent and selective peptidoleukotriene receptor antagonist in guinea pig and human airways

artículo científico publicado en 1987

Phosphodiesterase IV inhibitors as therapy for eosinophil-induced lung injury in asthma

artículo científico publicado en 1994

Phosphodiesterase isozymes: molecular targets for novel antiasthma agents

artículo científico publicado en 1998

Phosphodiesterases: the journey towards therapeutics

artículo científico publicado en 2000

Potential use of selective phosphodiesterase inhibitors in the treatment of asthma

artículo científico publicado el 1 de enero de 1991

Preliminary identification and role of phosphodiesterase isozymes in human basophils

artículo científico publicado el 15 de abril de 1992

Prolonged beta adrenoceptor stimulation up-regulates cAMP phosphodiesterase activity in human monocytes by increasing mRNA and protein for phosphodiesterases 4A and 4B

artículo científico publicado en 1996

Regulation of cAMP content and cAMP-dependent protein kinase activity in airway smooth muscle

artículo científico publicado en 1987

Role of conserved histidines in catalytic activity and inhibitor binding of human recombinant phosphodiesterase 4A

artículo científico publicado en 1997

Role of cyclic nucleotide phosphodiesterase isozymes in intact canine trachealis

artículo científico publicado el 1 de marzo de 1991

SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions

artículo científico publicado el 1 de enero de 1998

SK&F 104353, a selective leukotriene receptor antagonist, inhibits leukotriene D4- and antigen-induced bronchoconstriction in cynomolgus monkeys

artículo científico publicado el 1 de septiembre de 1992

Salbutamol up-regulates PDE4 activity and induces a heterologous desensitization of U937 cells to prostaglandin E2. Implications for the therapeutic use of beta-adrenoceptor agonists

artículo científico publicado en 1995

Stimulation of beta adrenoceptors in a human monocyte cell line (U937) up-regulates cyclic AMP-specific phosphodiesterase activity.

artículo científico publicado en 1992

Studies on β-adrenoceptors mediating changes in mechanical events and adenosine 3′,5′-monophosphate levels. Rat atria

artículo científico publicado el 1 de febrero de 1978

Suppression of human inflammatory cell function by subtype-selective PDE4 inhibitors correlates with inhibition of PDE4A and PDE4B.

artículo científico publicado en 1999

The bronchopulmonary pharmacology of SK&F; 104353 in anesthetized guinea pigs: demonstration of potent and selective antagonism of responses to peptidoleukotrienes

artículo científico publicado en 1989

The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one

scientific article published on 01 October 1993

The influence of endogenous catecholamines on the inhibitory effects of rolipram against early- and late-phase response to antigen in the guinea pig.

artículo científico publicado en 1997

The preclinical and clinical pharmacology of SK&F 104353, a potent and selective peptidoleukotriene receptor antagonist

artículo científico publicado en 1991

Therapeutic potential of isozyme-selective phosphodiesterase inhibitors in the treatment of asthma

artículo científico publicado el 1 de enero de 1992

What's in the pipeline? Prospects for monoclonal antibodies (mAbs) as therapies for lung diseases

artículo científico publicado en 2002