PAF receptor antagonists(Platelet activating factor receptor antagonists), PDE3 inhibitors(Phosphodiesterase 3 inhibitors), PDE4 inhibitors(Phosphodieterase 4 inhibitors)

Therapeutic Areas

Immune System DiseasesRespiratory Diseases

Active Indication-

Inactive Indication

Asthma

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis Pharma AG

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

Structure

Molecular FormulaC23H27N3O3

InChIKeyDCDXHGMCXGHXBM-YLBUIOQXSA-N

CAS Registry35135-01-4

View All Structures (2)

100 Clinical Results associated with Benafentrine dimaleate

100 Translational Medicine associated with Benafentrine dimaleate

100 Patents (Medical) associated with Benafentrine dimaleate

Literatures (Medical) associated with Benafentrine dimaleate

01 Jul 1998·European Journal of PharmacologyQ3 · MEDICINE

Phosphodiesterase inhibitors suppress α2-adrenoceptor-mediated 5-hydroxytryptamine release from tracheae of newborn rabbits

Q3 · MEDICINE

Article

Author: Wessler, Ignaz ; Racke, Kurt ; Freitag, Anke

The outflow of 5-hydroxytryptamine (5-HT) from isolated tracheae of newborn rabbits was determined by high pressure liquid chromatography with electrochemical detection. This 5-HT outflow reflects release from neuroendocrine epithelial cells of the airway mucosa, as previously shown. Phenylephrine, via alpha2B-adrenoceptors, caused a transient increase in 5-HT outflow, maximally by about 250%, an effect mediated by liberation of intracellular Ca2+, as previously shown. The non-selective phosphodiesterase inhibitor 2-isobutyl-1-methylxanthine (IBMX) concentration-dependently inhibited phenylephrine-induced 5-HT release (completely at 100 microM, IC50: 1.3 microM). Likewise, benzafentrine (inhibitor of phosphodiesterase 3 and 4) and siguazodan (inhibitor of phosphodiesterase 3) also almost completely inhibited phenylephrine-induced 5-HT release with IC50 values of 1.7 and 4.2 microM, respectively. Rolipram (inhibitor of phosphodiesterase 4), in a concentration of 10 microM, which exceeds more than 10-fold the reported IC50 for phosphodiesterase 4, did not significantly affect phenylephrine-induced 5-HT release. 5-HT release induced by depolarizing concentrations of K+ (45 mM), which largely depends on extracellular Ca2+, was not affected by IBMX. In conclusion, phosphodiesterases, with characteristics of phosphodiesterase 3, appear to play an important role in the control of cyclic nucleotide mediated inhibition of 5-HT release from neuroendocrine epithelial cells.

01 Feb 1998·Life SciencesQ3 · MEDICINE

The effect duration of selective phosphodiesterase inhibitors in the guinea pig

Q3 · MEDICINE

Article

Author: Pierpaolo Ferlenga ; Ermanno Moriggi ; Claudio Semeraro ; Clive P. Page ; Domenico Spina ; Ivano Biasini ; Francesco Marchini

The beta-adrenoceptor agonists, isoprenaline, salbutamol and salmeterol, the non-selective phosphodiesterase (PDE) isoenzyme inhibitors, theophylline, trequinsin; the PDE3 isoenzyme inhibitor, milrinone; the PDE3/4 isoenzyme inhibitor, benzafentrine; and the PDE4 isoenzyme inhibitors, denbufylline, nitraquazone, RP 73401, Ro-20-1724, rolipram and tibenelast all induced concentration-dependent reversal of prostaglandin F2alpha-induced contraction of guinea-pig superfused trachea in vitro. The relaxant response of the non-selective PDE isoenzyme inhibitor trequinsin was slow in onset and demonstrated very slow recovery, similar to that observed with the long-acting beta2-adrenoceptor agonist, salmeterol and the PDE4 inhibitor, RP 73401. The relaxant agonists also significantly reversed bombesin-induced bronchospasm in anaesthetised guinea-pigs and there was a highly significant correlation between the ability of drugs to reverse PGF2alpha-induced contraction of guinea-pig isolated trachea in vitro and bombesin-induced bronchoconstriction in vivo. Furthermore, both salmeterol and trequinsin demonstrated long lasting bronchodilator responses consistent with the in vitro data. These results show that PDE isoenzyme inhibitors demonstrate different pharmacodynamic profiles that is not determined by PDE4 inhibitory potency and indicate that other factors may be important in this regard.

01 Sep 1997·European Journal of PharmacologyQ3 · MEDICINE

Effects of SCA40 on bovine trachealis muscle and on cyclic nucleotide phosphodiesterases

Q3 · MEDICINE

Article

Author: Roger C. Small ; Tristan M. Pocock ; Robert W. Foster ; Lynne M. Isaac ; Alain Michel ; Peter Chiu ; Florence Laurent ; Pierre Antoine Bonnet ; Keith R F Elliott

While UK-93,928 (1-[[3-(6,9-dihydro-6-oxo-9-propyl-1H-purin-2-yl)-4-ethoxyphenyl] sulfonyl]-4-methylpiperazine; 5 nM-5 microM) was devoid of relaxant activity, benzafentrine, isoprenaline, levcromakalim and SCA40 (6-bromo-8-methylaminoimidazo[1,2-a]pyrazine-2-carbonitrile) each relaxed histamine (460 microM)-precontracted bovine isolated trachealis. Each of these relaxants was antagonised by a K+-rich (80 mM) medium. Except in the case of levcromakalim, nifedipine (1 microM) offset this antagonism. Charybdotoxin (100 nM) antagonised isoprenaline in a nifedipine-sensitive manner but did not antagonise SCA40 or benzafentrine. Iberiotoxin (100 nM) did not antagonise SCA40. Acting on tissue precontracted with carbachol, SCA40 potentiated isoprenaline but did not potentiate sodium nitroprusside. While levcromakalim (1 and 10 microM) induced hyperpolarisation, SCA40 (1 and 10 microM) induced little change in the membrane potential of bovine trachealis. In trachealis preloaded with 86Rb+, levcromakalim (1 and 10 microM) promoted efflux of the radiotracer while SCA40 (1 and 10 microM) had no effect. Tested as an inhibitor of isoenzymes of cyclic nucleotide phosphodiesterase, SCA40 was most potent against the type III, less potent against the type IV and least potent against the type I isoenzyme. It is concluded that neither inhibition of phosphodiesterase type V nor the promotion of BKCa channel opening explains the tracheal smooth muscle relaxant activity of SCA40. This compound relaxes bovine tracheal smooth muscle mainly by inhibiting phosphodiesterase isoenzyme types III and IV.

100 Deals associated with Benafentrine dimaleate

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 1	-	Novartis Pharma AG	-

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