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Volumn 318, Issue 2, 2006, Pages 840-848

The pharmacology of two novel long-acting phosphodiesterase 3/4 inhibitors, RPL554 [9,10-dimethoxy-2(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2- aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one] and RPL565 [6,7-dihydro-2-(2,6-diisopropylphenoxy)-9,10-dimethoxy-4H-pyrimido[6,1-a] isoquinolin-4-one]

Author keywords

[No Author keywords available]

Indexed keywords

[6,7 DIHYDRO 2 (2,6 DIISOPROPYLPHENOXY) 9,10 DIMETHOXY 4H PYRIMIDO(6,1A)ISOQUINOLIN 4 ONE]; [9,10 DIMETHOXY 2 (2,4,6 TRINETHYLPHENYLIMINO) 3 (N CARBAMOYL 2 AMINOETHYL) 3,4,6,7 TETRAHYDRO 2H PYRIMIDO(6,1A)ISOQUINOLIN 4 ONE]; HISTAMINE; LACTOSE; LONG ACTING DRUG; OVALBUMIN; PHOSPHODIESTERASE III INHIBITOR; PHOSPHODIESTERASE IV INHIBITOR; PHYTOHEMAGGLUTININ; PLASMA PROTEIN; TUMOR NECROSIS FACTOR ALPHA; UNCLASSIFIED DRUG;

EID: 33745939122     PISSN: 00223565     EISSN: 15210103     Source Type: Journal    
DOI: 10.1124/jpet.105.099192     Document Type: Article
Times cited : (88)

References (41)
  • 2
    • 0028824956 scopus 로고
    • The effect of selective phosphodiesterase inhibitors in comparison with other antiasthma drugs on allergen-induced eosinophilia in guinea-pig airways
    • Banner KH, Marchini F, Buschi A, Moriggi E, Semeraro C, and Page CP (1995) The effect of selective phosphodiesterase inhibitors in comparison with other antiasthma drugs on allergen-induced eosinophilia in guinea-pig airways. Pul Pharmacol 8:37-42.
    • (1995) Pul Pharmacol , vol.8 , pp. 37-42
    • Banner, K.H.1    Marchini, F.2    Buschi, A.3    Moriggi, E.4    Semeraro, C.5    Page, C.P.6
  • 3
    • 0031885147 scopus 로고    scopus 로고
    • Effect of selective phosphodiesterase 3 inhibition on the early and late asthmatic responses to inhaled allergen
    • Bardin PG, Doward MA, Lampe FC, Franke B, and Holgate ST (1998) Effect of selective phosphodiesterase 3 inhibition on the early and late asthmatic responses to inhaled allergen. Br J Clin Pharmacol 45:387-391.
    • (1998) Br J Clin Pharmacol , vol.45 , pp. 387-391
    • Bardin, P.G.1    Doward, M.A.2    Lampe, F.C.3    Franke, B.4    Holgate, S.T.5
  • 5
    • 0347082477 scopus 로고    scopus 로고
    • Roflumilast, a selective phosphodiesterase 4 inhibitor, shows efficacy and safety in the long-term treatment of asthma
    • Bateman ED, Izquirdo JL, Vetter N, Schmid-Wirlitsch C, and Bredenbroker D (2003) Roflumilast, a selective phosphodiesterase 4 inhibitor, shows efficacy and safety in the long-term treatment of asthma (Abstract). Eur Respir J 22 (Suppl 45):1393.
    • (2003) Eur Respir J , vol.22 , Issue.45 SUPPL. , pp. 1393
    • Bateman, E.D.1    Izquirdo, J.L.2    Vetter, N.3    Schmid-Wirlitsch, C.4    Bredenbroker, D.5
  • 6
    • 0035078823 scopus 로고    scopus 로고
    • In vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor
    • Bundschuh DS, Eltze M, Barsig J, Wollin L, Hatzelmann A, and Beume R (2001) In vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor. J Pharmacol Exp Ther 297:280-290.
    • (2001) J Pharmacol Exp Ther , vol.297 , pp. 280-290
    • Bundschuh, D.S.1    Eltze, M.2    Barsig, J.3    Wollin, L.4    Hatzelmann, A.5    Beume, R.6
  • 7
    • 0030128737 scopus 로고    scopus 로고
    • Isolated, electrically-stimulated airway preparations-their use in determining betaadrenoceptor agonist activity
    • Coleman RA, Nials AT, Rabe KF, Vardey CJ, and Watson N (1996) Isolated, electrically-stimulated airway preparations-their use in determining betaadrenoceptor agonist activity. Pulm Pharmacol 9:107-117.
    • (1996) Pulm Pharmacol , vol.9 , pp. 107-117
    • Coleman, R.A.1    Nials, A.T.2    Rabe, K.F.3    Vardey, C.J.4    Watson, N.5
  • 8
    • 0027535918 scopus 로고
    • Investigation into the role of phosphodiesterase IV in bronchorelaxation, including studies with human bronchus
    • Cortijo J, Bou J, Beleta J, Cardelus I, Llenas J, Morcillo E, and Gristwood RW (1993) Investigation into the role of phosphodiesterase IV in bronchorelaxation, including studies with human bronchus. Br J Pharmacol 108:562-568.
    • (1993) Br J Pharmacol , vol.108 , pp. 562-568
    • Cortijo, J.1    Bou, J.2    Beleta, J.3    Cardelus, I.4    Llenas, J.5    Morcillo, E.6    Gristwood, R.W.7
  • 9
    • 0029881921 scopus 로고    scopus 로고
    • Phosphodiesterase inhibitors suppress proliferation of peripheral blood mononuclear cells and interleukin-4 and -5 secretion by human T-helper type 2 cells
    • Crocker IC, Townley RG, and Khan MM (1996) Phosphodiesterase inhibitors suppress proliferation of peripheral blood mononuclear cells and interleukin-4 and -5 secretion by human T-helper type 2 cells. Immunopharmacology 31:223-235.
    • (1996) Immunopharmacology , vol.31 , pp. 223-235
    • Crocker, I.C.1    Townley, R.G.2    Khan, M.M.3
  • 10
    • 0026741623 scopus 로고
    • Human bronchial cyclic nucleotide phosphodiesterase isoenzymes: Biochemical and pharmacological analysis using selective inhibitors
    • de Boer J, Philpott AJ, Van Amsterdam RG, Shahid M, Zaagsma J, and Nicholson CD (1992) Human bronchial cyclic nucleotide phosphodiesterase isoenzymes: biochemical and pharmacological analysis using selective inhibitors. Br J Pharmacol 106:1028-1034.
    • (1992) Br J Pharmacol , vol.106 , pp. 1028-1034
    • De Boer, J.1    Philpott, A.J.2    Van Amsterdam, R.G.3    Shahid, M.4    Zaagsma, J.5    Nicholson, C.D.6
  • 11
    • 0035188826 scopus 로고    scopus 로고
    • Cyclic nucleotide phosphodiesterases
    • Essayan DM (2001) Cyclic nucleotide phosphodiesterases. J Allergy Clin Immunol 108:671-680.
    • (2001) J Allergy Clin Immunol , vol.108 , pp. 671-680
    • Essayan, D.M.1
  • 12
    • 0024535842 scopus 로고
    • Regional and time-dependent effects of inflammatory mediators on airway microvascular permeability in the guinea pig
    • Evans TW, Rogers DF, Aursudkij B, Chung KF, and Barnes PJ (1989) Regional and time-dependent effects of inflammatory mediators on airway microvascular permeability in the guinea pig. Clin Sci (Lond) 76:479-485.
    • (1989) Clin Sci (Lond) , vol.76 , pp. 479-485
    • Evans, T.W.1    Rogers, D.F.2    Aursudkij, B.3    Chung, K.F.4    Barnes, P.J.5
  • 14
    • 0029868922 scopus 로고    scopus 로고
    • Effects of theophylline and rolipram on antigen-induced airway responses in neonatally immunized rabbits
    • Gozzard N, Herd CM, Blake SM, Holbrook M, Hughes B, Higgs GA, and Page CP (1996) Effects of theophylline and rolipram on antigen-induced airway responses in neonatally immunized rabbits. Br J Pharmacol 117:1405-1412.
    • (1996) Br J Pharmacol , vol.117 , pp. 1405-1412
    • Gozzard, N.1    Herd, C.M.2    Blake, S.M.3    Holbrook, M.4    Hughes, B.5    Higgs, G.A.6    Page, C.P.7
  • 15
    • 0037350231 scopus 로고    scopus 로고
    • Does a single dose of the phosphodiesterase 4 inhibitor, cilomilast (15 mg), induce bronchodilation in patients with chronic obstructive pulmonary disease?
    • Grootendorst DC, Gauw SA, Baan R, Kelly J, Murdoch RD, Sterk PJ, and Rabe KF (2003) Does a single dose of the phosphodiesterase 4 inhibitor, cilomilast (15 mg), induce bronchodilation in patients with chronic obstructive pulmonary disease? Pulm Pharmacol Ther 16:115-120.
    • (2003) Pulm Pharmacol Ther , vol.16 , pp. 115-120
    • Grootendorst, D.C.1    Gauw, S.A.2    Baan, R.3    Kelly, J.4    Murdoch, R.D.5    Sterk, P.J.6    Rabe, K.F.7
  • 16
    • 0035084103 scopus 로고    scopus 로고
    • Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro
    • Hatzelmann A and Schudt C (2001) Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther 297:267-279.
    • (2001) J Pharmacol Exp Ther , vol.297 , pp. 267-279
    • Hatzelmann, A.1    Schudt, C.2
  • 17
    • 0027440329 scopus 로고
    • Comparative effects of caffeine and selective phosphodiesterase inhibitors on respiration and behavior in rhesus monkeys
    • Howell LL (1993) Comparative effects of caffeine and selective phosphodiesterase inhibitors on respiration and behavior in rhesus monkeys. J Pharmacol Exp Ther 266:894-903.
    • (1993) J Pharmacol Exp Ther , vol.266 , pp. 894-903
    • Howell, L.L.1
  • 18
    • 8944247744 scopus 로고    scopus 로고
    • The inhibition of antigen-induced eosinophilia and bronchoconstriction by CDP840, a novel stereo-selective inhibitor of phosphodiesterase type 4
    • Hughes B, Howat D, Lisle H, Holbrook M, James T, Gozzard N, Blease K, Hughes P, Kingaby R, Warrellow G, et al. (1996) The inhibition of antigen-induced eosinophilia and bronchoconstriction by CDP840, a novel stereo-selective inhibitor of phosphodiesterase type 4. Br J Pharmacol 118:1183-1191.
    • (1996) Br J Pharmacol , vol.118 , pp. 1183-1191
    • Hughes, B.1    Howat, D.2    Lisle, H.3    Holbrook, M.4    James, T.5    Gozzard, N.6    Blease, K.7    Hughes, P.8    Kingaby, R.9    Warrellow, G.10
  • 19
    • 11844249945 scopus 로고    scopus 로고
    • The effect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro
    • Jones NA, Boswell-Smith V, Lever R, and Page CP (2005) The effect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro. Pulm Pharmacol Ther 18:93-101.
    • (2005) Pulm Pharmacol Ther , vol.18 , pp. 93-101
    • Jones, N.A.1    Boswell-Smith, V.2    Lever, R.3    Page, C.P.4
  • 20
    • 0141630489 scopus 로고    scopus 로고
    • In vivo efficacy in airway disease models of N-(3,5-dichloropyrid-4-yl)- [1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), a selective phosphodiesterase 4 inhibitor for inhaled administration
    • Kuss H, Hoefgen N, Johanssen S, Kronbach T, and Rundfeldt C (2003) In vivo efficacy in airway disease models of N-(3,5-dichloropyrid-4-yl)-[1-(4- fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), a selective phosphodiesterase 4 inhibitor for inhaled administration. J Pharmacol Exp Ther 307:373-385.
    • (2003) J Pharmacol Exp Ther , vol.307 , pp. 373-385
    • Kuss, H.1    Hoefgen, N.2    Johanssen, S.3    Kronbach, T.4    Rundfeldt, C.5
  • 21
    • 11844267183 scopus 로고    scopus 로고
    • Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease
    • Lipworth BJ (2005) Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease. Lancet 365:167-175.
    • (2005) Lancet , vol.365 , pp. 167-175
    • Lipworth, B.J.1
  • 22
    • 29144531153 scopus 로고    scopus 로고
    • Safety of long-acting beta-agonists: An urgent need to clear the air
    • Martinez FD (2005) Safety of long-acting beta-agonists: an urgent need to clear the air. N Engl J Med 353:2637-2639.
    • (2005) N Engl J Med , vol.353 , pp. 2637-2639
    • Martinez, F.D.1
  • 24
    • 0029831004 scopus 로고    scopus 로고
    • Effects of RP 73401, a novel, potent and selective phosphodiesterase type 4 inhibitor, on contractility of human, isolated bronchial muscle
    • Naline E, Qian Y, Advenier C, Raeburn D, and Karlsson JA (1996) Effects of RP 73401, a novel, potent and selective phosphodiesterase type 4 inhibitor, on contractility of human, isolated bronchial muscle. Br J Pharmacol 118:1939-1944.
    • (1996) Br J Pharmacol , vol.118 , pp. 1939-1944
    • Naline, E.1    Qian, Y.2    Advenier, C.3    Raeburn, D.4    Karlsson, J.A.5
  • 25
    • 0030051755 scopus 로고    scopus 로고
    • Effects of selective phosphodiesterase inhibitors on platelet-activating factor- and antigeninduced airway hyperreactivity, eosinophil accumulation and microvascular leakage in guinea pigs
    • Ortiz JL, Valles JM, Marti-Cabrera M, Cortijo J, and Morcillo EJ (1996) Effects of selective phosphodiesterase inhibitors on platelet-activating factor- and antigeninduced airway hyperreactivity, eosinophil accumulation and microvascular leakage in guinea pigs. Naunyn-Schmiedeberg's Arch Pharmacol 353:200-206.
    • (1996) Naunyn-Schmiedeberg's Arch Pharmacol , vol.353 , pp. 200-206
    • Ortiz, J.L.1    Valles, J.M.2    Marti-Cabrera, M.3    Cortijo, J.4    Morcillo, E.J.5
  • 26
    • 33745954246 scopus 로고    scopus 로고
    • inventor, Vernalis Ltd, assignee. Derivatives of pyrimido [6-1-A] isoquinolin-4-one. U.S. patent 200417182, 2004 Sept. 21
    • Oxford AW and Jack D (2004) inventor, Vernalis Ltd, assignee. Derivatives of pyrimido [6-1-A] isoquinolin-4-one. U.S. patent 200417182, 2004 Sept. 21.
    • (2004)
    • Oxford, A.W.1    Jack, D.2
  • 28
    • 0029072842 scopus 로고
    • Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants
    • Rabe KF, Magnussen H, and Dent G (1995) Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants. Eur Respir J 8:637-642.
    • (1995) Eur Respir J , vol.8 , pp. 637-642
    • Rabe, K.F.1    Magnussen, H.2    Dent, G.3
  • 29
    • 0027267644 scopus 로고
    • Isoenzyme-selective cyclic nucleotide phosphodiesterase inhibitors: Biochemistry, pharmacology and therapeutic potential in asthma
    • Raeburn D, Souness JE, Tomkinson A, and Karlsson JA (1993) Isoenzyme-selective cyclic nucleotide phosphodiesterase inhibitors: biochemistry, pharmacology and therapeutic potential in asthma. Prog Drug Res 40:9-32.
    • (1993) Prog Drug Res , vol.40 , pp. 9-32
    • Raeburn, D.1    Souness, J.E.2    Tomkinson, A.3    Karlsson, J.A.4
  • 31
    • 0028970860 scopus 로고
    • Role of lipoxygenase metabolites in platelet-activating factor- and antigen-induced bronchial hyperresponsiveness and eosinophil infiltration
    • Seeds EA, Kilfeather S, Okiji S, Schoupe TS, Donigi-Gale D, and Page CP (1995) Role of lipoxygenase metabolites in platelet-activating factor- and antigen-induced bronchial hyperresponsiveness and eosinophil infiltration. Eur J Pharmacol 293:369-376.
    • (1995) Eur J Pharmacol , vol.293 , pp. 369-376
    • Seeds, E.A.1    Kilfeather, S.2    Okiji, S.3    Schoupe, T.S.4    Donigi-Gale, D.5    Page, C.P.6
  • 33
    • 4444330207 scopus 로고    scopus 로고
    • The potential of PDE4 inhibitors in respiratory disease
    • Spina D (2004) The potential of PDE4 inhibitors in respiratory disease. Curr Drug Targets Inflamm Allergy 3:231-236.
    • (2004) Curr Drug Targets Inflamm Allergy , vol.3 , pp. 231-236
    • Spina, D.1
  • 35
    • 0028787061 scopus 로고
    • Regulation by phosphodiesterase isoenzymes of non-adrenergic non-cholinergic contraction in guinea-pig isolated main bronchus
    • Spina D, Harrison S, and Page CP (1995) Regulation by phosphodiesterase isoenzymes of non-adrenergic non-cholinergic contraction in guinea-pig isolated main bronchus. Br J Pharmacol 116:2334-2340.
    • (1995) Br J Pharmacol , vol.116 , pp. 2334-2340
    • Spina, D.1    Harrison, S.2    Page, C.P.3
  • 36
    • 0141888498 scopus 로고    scopus 로고
    • Resolution of the oedema associated with allergic pulmonary inflammation in rats assessed noninvasively by magnetic resonance imaging
    • Tigani B, Cannet C, Zurbrugg S, Schaeublin E, Mazzoni L, Fozard JR, and Beckmann N (2003) Resolution of the oedema associated with allergic pulmonary inflammation in rats assessed noninvasively by magnetic resonance imaging. Br J Pharmacol 140:239-246.
    • (2003) Br J Pharmacol , vol.140 , pp. 239-246
    • Tigani, B.1    Cannet, C.2    Zurbrugg, S.3    Schaeublin, E.4    Mazzoni, L.5    Fozard, J.R.6    Beckmann, N.7
  • 37
    • 0031914520 scopus 로고    scopus 로고
    • Phosphodiesterase isoenzymes: Molecular targets for novel antiasthma agents
    • Torphy TJ (1998) Phosphodiesterase isoenzymes: molecular targets for novel antiasthma agents. Am J Respir Crit Care Med 157:351-370.
    • (1998) Am J Respir Crit Care Med , vol.157 , pp. 351-370
    • Torphy, T.J.1
  • 38
    • 0023819429 scopus 로고
    • Inhibition of the low km cyclic AMP phosphodiesterase in intact canine trachealis by SK&F 94836: Mechanical and biochemical responses
    • Torphy TJ, Burman M, Huang LB, and Tucker SS (1988) Inhibition of the low km cyclic AMP phosphodiesterase in intact canine trachealis by SK&F 94836: mechanical and biochemical responses. J Pharmacol Exp Ther 246:843-850.
    • (1988) J Pharmacol Exp Ther , vol.246 , pp. 843-850
    • Torphy, T.J.1    Burman, M.2    Huang, L.B.3    Tucker, S.S.4
  • 39
    • 0025868447 scopus 로고
    • Phosphodiesterase inhibitors: New opportunities for the treatment of asthma
    • Torphy TJ and Undem BJ (1991) Phosphodiesterase inhibitors: new opportunities for the treatment of asthma. Thorax 46:512-523.
    • (1991) Thorax , vol.46 , pp. 512-523
    • Torphy, T.J.1    Undem, B.J.2
  • 41
    • 0028289793 scopus 로고
    • Comparison of phosphodiesterase III, IV and dual III/IV inhibitors on bronchospasm and pulmonary eosinophil influx in guinea pigs
    • Underwood DC, Kotzer CJ, Bochnowicz S, Osborn RR, Luttmann MA, Hay DW, and Torphy TJ (1994) Comparison of phosphodiesterase III, IV and dual III/IV inhibitors on bronchospasm and pulmonary eosinophil influx in guinea pigs. J Pharmacol Exp Ther 270:250-259.
    • (1994) J Pharmacol Exp Ther , vol.270 , pp. 250-259
    • Underwood, D.C.1    Kotzer, C.J.2    Bochnowicz, S.3    Osborn, R.R.4    Luttmann, M.A.5    Hay, D.W.6    Torphy, T.J.7


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