Page last updated: 2024-11-04

rolipram and Emesis

rolipram has been researched along with Emesis in 25 studies

Research Excerpts

ExcerptRelevanceReference
"C57Bl/6J male mice were used to compare the effect of three doses of free and FLV-delivered (FLVs-Rol) rolipram in a behavioral correlate model of rolipram-induced emesis."8.12Novel Liposomal Rolipram Formulation for Clinical Application to Reduce Emesis. ( Barve, S; Bauer, P; Gobejishvili, L; Lydic, T; Maldonado, C; McClain, C; Rodriguez, WE; Soni, C; Wang, Y, 2022)
"C57Bl/6J male mice were used to compare the effect of three doses of free and FLV-delivered (FLVs-Rol) rolipram in a behavioral correlate model of rolipram-induced emesis."4.12Novel Liposomal Rolipram Formulation for Clinical Application to Reduce Emesis. ( Barve, S; Bauer, P; Gobejishvili, L; Lydic, T; Maldonado, C; McClain, C; Rodriguez, WE; Soni, C; Wang, Y, 2022)
"Using tumor necrosis factor (TNF) inhibition in dog blood as a measure of efficacy, and canine emesis as a measure of toxicity, we were able to assign a therapeutic index to rolipram, a prototypic anti-inflammatory compound."3.69A canine model for determination of the therapeutic index of cytokine inhibitors. ( Baer, P; Clifton, L; Connolly, KM; Dennis, S; Han, B; Numerick, MJ; Sekut, L; Silverstein, R; Verghese, MW, 1995)
" Concerns regarding its long-term use particularly in young children has provided an impetus for discovering novel anti-inflammatory molecules with high tolerability and clinical efficacy."2.42The potential of PDE4 inhibitors in respiratory disease. ( Spina, D, 2004)
" Substitution at the 3-position of the 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridine tricycle led to a 2-thienyl analog, 19 (tofimilast), a potent PDE4 inhibitor with low oral bioavailability and no emesis-associated behaviors in ferrets at plasma concentrations up to 152 ng/mL."1.34SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase. ( Bachert, EL; Cheng, JB; Cohan, VL; Duplantier, AJ; Jenkinson, TH; Kraus, KG; McKechney, MW; Pillar, JD; Watson, JW, 2007)
" Emesis induced by RS14203 exhibited a dose-response relationship but no such relationship was seen for R-rolipram or CT-2450."1.30Emesis induced by inhibitors of type IV cyclic nucleotide phosphodiesterase (PDE IV) in the ferret. ( Choudhury, I; Robichaud, A; Rodger, IW; Tattersall, FD, 1999)
"Rolipram was characterized for its emetic, behavioral, cardiovascular and pulmonary activities in dogs, to assess its systemic pharmacology and potential bronchodilatory selectivity."1.29Emetic, central nervous system, and pulmonary activities of rolipram in the dog. ( Evans, DY; Heaslip, RJ, 1995)

Research

Studies (25)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's8 (32.00)18.2507
2000's12 (48.00)29.6817
2010's3 (12.00)24.3611
2020's2 (8.00)2.80

Authors

AuthorsStudies
Duplantier, AJ2
Biggers, MS1
Chambers, RJ1
Cheng, JB2
Cooper, K1
Damon, DB1
Eggler, JF1
Kraus, KG2
Marfat, A1
Masamune, H1
Pillar, JS1
Shirley, JT1
Umland, JP1
Watson, JW2
He, W1
Huang, FC1
Hanney, B1
Souness, J1
Miller, B1
Liang, G1
Mason, J1
Djuric, S1
Montana, JG2
Cooper, N2
Dyke, HJ2
Gowers, L2
Gregory, JP1
Hellewell, PG2
Miotla, J1
Morris, K1
Naylor, R2
Tuladhar, B1
Warneck, JB2
Ukita, T1
Sugahara, M1
Terakawa, Y1
Kuroda, T1
Wada, K1
Nakata, A1
Ohmachi, Y1
Kikkawa, H1
Ikezawa, K1
Naito, K1
Buckley, G1
Galleway, F1
Gregory, JC1
Hannah, DR1
Haughan, AF1
Kendall, HJ1
Lowe, C1
Maxey, R1
Picken, CL1
Runcie, KA1
Sabin, V1
Tuladhar, BR1
Macdonald, D1
Perrier, H1
Liu, S1
Laliberté, F1
Rasori, R1
Robichaud, A3
Masson, P1
Huang, Z1
Burnouf, C1
Auclair, E1
Avenel, N1
Bertin, B1
Bigot, C1
Calvet, A1
Chan, K1
Durand, C1
Fasquelle, V1
Féru, F1
Gilbertsen, R1
Jacobelli, H1
Kebsi, A1
Lallier, E1
Maignel, J1
Martin, B1
Milano, S1
Ouagued, M1
Pascal, Y1
Pruniaux, MP1
Puaud, J1
Rocher, MN1
Terrasse, C1
Wrigglesworth, R1
Doherty, AM1
Kim, E1
Chun, HO1
Jung, SH1
Kim, JH1
Lee, JM1
Suh, BC1
Xiang, MX1
Rhee, CK1
Bachert, EL1
Cohan, VL1
Jenkinson, TH1
McKechney, MW1
Pillar, JD1
García, AM1
Brea, J1
Morales-García, JA1
Perez, DI1
González, A1
Alonso-Gil, S1
Gracia-Rubio, I1
Ros-Simó, C1
Conde, S1
Cadavid, MI1
Loza, MI1
Perez-Castillo, A1
Valverde, O1
Martinez, A1
Gil, C1
Liang, J1
Huang, YY1
Zhou, Q1
Gao, Y1
Li, Z1
Wu, D1
Yu, S1
Guo, L1
Chen, Z1
Huang, L1
Liang, SH1
He, X1
Wu, R1
Luo, HB1
Gobejishvili, L1
Rodriguez, WE1
Bauer, P1
Wang, Y1
Soni, C1
Lydic, T1
Barve, S1
McClain, C1
Maldonado, C1
Vanmierlo, T1
Creemers, P1
Akkerman, S1
van Duinen, M1
Sambeth, A1
De Vry, J1
Uz, T1
Blokland, A1
Prickaerts, J1
Zhou, ZZ1
Cheng, YF1
Zou, ZQ1
Ge, BC1
Yu, H1
Huang, C1
Wang, HT1
Yang, XM1
Xu, JP1
Dastidar, SG1
Ray, A1
Shirumalla, R1
Rajagopal, D1
Chaudhary, S1
Nanda, K1
Sharma, P1
Seth, MK1
Balachandran, S1
Gupta, N1
Palle, V1
Davis, TG1
Peterson, JJ1
Kou, JP1
Capper-Spudich, EA1
Ball, D1
Nials, AT1
Wiseman, J1
Solanke, YE1
Lucas, FS1
Williamson, RA1
Ferrari, L1
Wren, P1
Knowles, RG1
Barnette, MS2
Podolin, PL1
Ochiai, H1
Odagaki, Y1
Ohtani, T1
Ishida, A1
Kusumi, K1
Kishikawa, K1
Yamamoto, S1
Takeda, H1
Obata, T1
Kobayashi, K1
Nakai, H1
Toda, M1
Spina, D1
Hirose, R1
Manabe, H1
Nonaka, H1
Yanagawa, K1
Akuta, K1
Sato, S1
Ohshima, E1
Ichimura, M1
Heaslip, RJ1
Evans, DY1
Sekut, L1
Han, B1
Baer, P1
Verghese, MW1
Silverstein, R1
Clifton, L1
Dennis, S1
Numerick, MJ1
Connolly, KM1
Christensen, SB1
Guider, A1
Forster, CJ1
Gleason, JG1
Bender, PE1
Karpinski, JM1
DeWolf, WE1
Underwood, DC1
Griswold, DE1
Cieslinski, LB1
Burman, M1
Bochnowicz, S1
Osborn, RR1
Manning, CD1
Grous, M1
Hillegas, LM1
Bartus, JO1
Ryan, MD1
Eggleston, DS1
Haltiwanger, RC1
Torphy, TJ1
Tattersall, FD2
Choudhury, I1
Rodger, IW1
Savoie, C1
Stamatiou, PB1
Chan, CC1
Aoki, M1
Fukunaga, M1
Sugimoto, T1
Hirano, Y1
Kobayashi, M1
Honda, K1
Yamada, T1

Reviews

1 review available for rolipram and Emesis

ArticleYear
The potential of PDE4 inhibitors in respiratory disease.
    Current drug targets. Inflammation and allergy, 2004, Volume: 3, Issue:3

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Anti-Inflammatory Agents; Bronchodilator Agents; Clinical Trial

2004

Other Studies

24 other studies available for rolipram and Emesis

ArticleYear
Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.
    Journal of medicinal chemistry, 1996, Jan-05, Volume: 39, Issue:1

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Benzoates; Binding Sites; Brain; Cyclic Nucleotide Pho

1996
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
    Journal of medicinal chemistry, 1998, Oct-22, Volume: 41, Issue:22

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Anti-Inflammatory Agents, Non-Steroidal; Benzamides; B

1998
PDE4 inhibitors: new xanthine analogues.
    Bioorganic & medicinal chemistry letters, 1998, Oct-20, Volume: 8, Issue:20

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Cyclic Nucleotide Phosphodiesterases, Type 4; Eosinoph

1998
Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.
    Journal of medicinal chemistry, 1999, Mar-25, Volume: 42, Issue:6

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Anti-Asthmatic Agents; Binding, Competitive; Brain; Br

1999
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.
    Bioorganic & medicinal chemistry letters, 2000, Sep-18, Volume: 10, Issue:18

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Administration, Oral; Animals; Asthma; Benzamides; Benzofurans;

2000
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
    Journal of medicinal chemistry, 2000, Oct-19, Volume: 43, Issue:21

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Anti-Asthmatic Agents; Azides; Bronchoconstriction; Ce

2000
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.
    Journal of medicinal chemistry, 2000, Dec-14, Volume: 43, Issue:25

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; 3',5'-Cyclic-GMP Phosphodiesterases; Animals; Anti-Asthmatic Ag

2000
Improvement of therapeutic index of phosphodiesterase type IV inhibitors as anti-Asthmatics.
    Bioorganic & medicinal chemistry letters, 2003, Jul-21, Volume: 13, Issue:14

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Anti-Asthmatic Agents; Binding Sites; Brain; Bronchoal

2003
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
    Journal of medicinal chemistry, 2007, Jan-25, Volume: 50, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Biological Availability; Cyclic Nucleotide Phosphodies

2007
Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.
    Journal of medicinal chemistry, 2014, Oct-23, Volume: 57, Issue:20

    Topics: Anesthesia; Animals; Anti-Inflammatory Agents, Non-Steroidal; Blood-Brain Barrier; Cell Survival; Ch

2014
Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.
    Journal of medicinal chemistry, 2020, 03-26, Volume: 63, Issue:6

    Topics: Aminopyridines; Animals; Benzamides; Cyclic Nucleotide Phosphodiesterases, Type 4; Cyclopropanes; De

2020
Novel Liposomal Rolipram Formulation for Clinical Application to Reduce Emesis.
    Drug design, development and therapy, 2022, Volume: 16

    Topics: Animals; Chromatography, Liquid; Male; Mice; Mice, Inbred C57BL; Phosphodiesterase 4 Inhibitors; Rol

2022
The PDE4 inhibitor roflumilast improves memory in rodents at non-emetic doses.
    Behavioural brain research, 2016, Apr-15, Volume: 303

    Topics: Aminopyridines; Animals; Benzamides; Cyclopropanes; Donepezil; Indans; Male; Memory; Mice; Mice, Inb

2016
Discovery of N-Alkyl Catecholamides as Selective Phosphodiesterase-4 Inhibitors with Anti-neuroinflammation Potential Exhibiting Antidepressant-like Effects at Non-emetic Doses.
    ACS chemical neuroscience, 2017, 01-18, Volume: 8, Issue:1

    Topics: Animals; Anti-Inflammatory Agents; Antidepressive Agents; Cyclic Nucleotide Phosphodiesterases, Type

2017
Pharmacology of a novel, orally active PDE4 inhibitor.
    Pharmacology, 2009, Volume: 83, Issue:5

    Topics: Animals; Carboxylic Acids; Cell Line, Transformed; Cyclic AMP; Cyclohexanecarboxylic Acids; Disease

2009
The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in
    The Journal of pharmacology and experimental therapeutics, 2009, Volume: 330, Issue:3

    Topics: Aminopyridines; Animals; Benzamides; Carboxylic Acids; Cyclohexanecarboxylic Acids; Cyclopropanes; F

2009
Design, synthesis, and biological evaluation of new phosphodiesterase type 4 inhibitors.
    Bioorganic & medicinal chemistry, 2004, Oct-01, Volume: 12, Issue:19

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Binding Sites; Bronchoconstriction; Computer Simulatio

2004
Correlation between emetic effect of phosphodiesterase 4 inhibitors and their occupation of the high-affinity rolipram binding site in Suncus murinus brain.
    European journal of pharmacology, 2007, Nov-14, Volume: 573, Issue:1-3

    Topics: Animals; Benzamides; Binding Sites; Binding, Competitive; Brain; Dose-Response Relationship, Drug; I

2007
Emetic, central nervous system, and pulmonary activities of rolipram in the dog.
    European journal of pharmacology, 1995, Nov-24, Volume: 286, Issue:3

    Topics: Animals; Anxiety; Asthma; Brain; Bronchi; Dogs; Female; Heart Rate; Male; Nadolol; Pentobarbital; Ph

1995
A canine model for determination of the therapeutic index of cytokine inhibitors.
    Laboratory animal science, 1995, Volume: 45, Issue:6

    Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Cells, Cultured; Dogs; Dose-Response Relationship,

1995
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
    Journal of medicinal chemistry, 1998, Mar-12, Volume: 41, Issue:6

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Anti-Asthmatic Agents; Anti-Inflammatory Agents, Non-S

1998
Emesis induced by inhibitors of type IV cyclic nucleotide phosphodiesterase (PDE IV) in the ferret.
    Neuropharmacology, 1999, Volume: 38, Issue:2

    Topics: Animals; Antiemetics; Dose-Response Relationship, Drug; Emetics; Ferrets; Indoles; Molecular Structu

1999
PDE4 inhibitors induce emesis in ferrets via a noradrenergic pathway.
    Neuropharmacology, 2001, Volume: 40, Issue:2

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Adrenergic alpha-Agonists; Adrenergic alpha-Antagonists; Anesth

2001
Studies on mechanisms of low emetogenicity of YM976, a novel phosphodiesterase type 4 inhibitor.
    The Journal of pharmacology and experimental therapeutics, 2001, Volume: 298, Issue:3

    Topics: 3',5'-Cyclic-AMP Phosphodiesterases; Animals; Body Temperature; Brain Chemistry; Cyclic Nucleotide P

2001
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