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Aminophylline

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Chemical Structure| 317-34-0 同义名 : Phyllocontin
CAS号 : 317-34-0
货号 : A594330
分子式 : C16H24N10O4
纯度 : 98+%
分子量 : 420.426
MDL号 : MFCD00013221
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(35.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 6 mg/mL(14.27 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • PDE

    PDE, IC50:0.12 mM
描述 Intracellular cyclic nucleotide levels can be controlled through regulation of either synthesis via respective cyclases or degradation via the phosphodiesterases (PDEs)[3]. Theophylline, a methylxanthine cyclic adenosine 3'5' monophosphate phosphodiesterase inhibitor, increases intracellular cAMP content and also stimulates fetal lung surfactant synthesis. Aminophylline is the ethylene diamine salt of theophylline[4]. It establishes capabilities to inhibit the cyclic AMP phosphodiesterase and cyclic GMP phosphodiesterase from human lung with I50 values of 0.16 mM and 0.138 mM at 1 μM cyclic AMP and 1 μM cyclic GMP, respectively[3]. Treatment with aminophylline for 24 hours resulted in a 25% (P less than 0.025) decrease in the glycogen content of the explants and glycogen synthase I activity was reduced by 32% in aminophylline treated cultures (P < 0.025)[4]. At higher concentrations (1 and 5 mM), aminophylline significantly elevated the basal cyclic AMP levels of the mouse vas deferens and markedly inhibited the contractile response to various frequencies of stimulation[5]. In five normal and five asthmatic subjects, the plasma cyclic AMP response to isoprenaline aerosol inhalation was enhanced by aminophylline, although to a lesser degree in the asthmatic subjects[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03296202 - Recruiting July 2021 France ... 展开 >> service de médecine interne - CH d'Agen Not yet recruiting Agen, France, 47923 Contact: Patrick RISPAL, MD       rispalp@ch-agen.fr    Principal Investigator: Patrick RISPAL, MD          service de maladies infectieuses - CH de la Côte Basque Recruiting Bayonne, France, 64109 Contact: Marc-Olivier VAREIL, MD       movareil@ch-cotebasque.fr    Principal Investigator: Marc-Olivier VAREIL, MD          service de médecine inter et maladies infectieuses - Hopital Saint André Recruiting Bordeaux, France, 33075 Contact: Patrick MERCIE, Prof       patrick.mercie@chu-bordeaux.fr    Principal Investigator: Patrick MERCIE, Prof          service de médecine interne et maladies infectieuses - Hôpital Saint-André Recruiting Bordeaux, France, 33075 Contact: Fabrice BONNET, Prof       fabrice.bonnet@chu-bordeaux.fr    Principal Investigator: Fabrice BONNET, Prof          service de maladies infectieuses et médecine tropicale - Hôpital Pellegrin Recruiting Bordeaux, France, 33076 Contact: MALVY Denis, Prof       denis.malvy@chu-bordeaux.fr    Principal Investigator: Denis MALVY, Prof          service de maladies infectieuses et médecine tropicale - Hôpital Pellegrin Recruiting Bordeaux, France, 33076 Contact: Didier NEAU, Prof       didier.neau@chu-bordeaux.fr    Principal Investigator: Didier NEAU, Prof          service de maladies infectieuses et médecine tropicale - Hôpital Pellegrin Recruiting Bordeaux, France, 33076 Contact: DUPON Michel, Prof       michel.dupon@chu-bordeaux.fr    Principal Investigator: DUPON Michel, Prof          Service D'Urgences Pédiatriques Recruiting Bordeaux, France Contact: Camille RUNEL-BELLIARD, MD       camille.runel@chu-bordeaux.fr    Principal Investigator: Camille RUNEL-BELLIARD, MD          service de médecine interne et maladies infectieuses - CH de Dax Recruiting Dax, France, 40107 Contact: Yann GERARD, MD       gerardy@ch-dax.fr    Principal Investigator: Yann GERARD, MD          service de médecine interne - CH d'Arcachon Recruiting La Teste-de-Buch, France, 33260 Contact: Carine COURTAULT, MD       carine.courtault@ch-arcachon.fr    Principal Investigator: Carine COURTAULT, MD          service de médecine interne - CH de Libourne Not yet recruiting Libourne, France, 33505 Contact: Helene FERRAND, MD       helene.ferrand@ch-libourne.fr    Sub-Investigator: Sten DE WITTE, MD          Principal Investigator: Helene FERRAND, MD          service de médecine interne - CH de Mont de Marsan Not yet recruiting Mont-de-Marsan, France, 40024 Contact: Maud FOISSAC, MD       maud.foissac@ch-mt-marsan.fr    Principal Investigator: Maud FOISSAC, MD          service de médecine interne - CH d'Orthez Recruiting Orthez, France Contact: Yann GERARD, MD       gerardy@ch-dax.fr    Principal Investigator: Yann GERARD, MD          service de médecine interne et maladies infectieuses - CH de Pau Recruiting Pau, France, 64000 Contact: Eric MONLUN, MD       eric.monlun@ch-pau.fr    Principal Investigator: Eric MONLUN, MD          service de médecine interne et maladies infectieuses - CH de Périgueux Recruiting Perigueux, France, 24019 Contact: Philippe LATASTE, MD       philippe.lataste@ch-perigueux.fr    Principal Investigator: Philippe LATASTE, MD          service de médecine interne et maladies infectieuses - Groupe hospitalier Sud Recruiting Pessac, France Contact: Jean-François VIALLARD, Prof       jean-francois.viallard@chu-bordeaux.fr    Sub-Investigator: Jean-Luc PELLEGRIN, Prof          Principal Investigator: Jean-François VIALLARD, Prof          service de maladies infecteieuses - CH Saint-Cyr Not yet recruiting Villeneuve sur Lot, France, 47307 Contact: Isabelle CHOSSAT, MD       isabelle.chossat@ch-stcyr.fr    Principal Investigator: Isabelle CHOSSAT, MD 收起 <<
NCT02997605 RheumatoId Arthritis Phase 4 Recruiting December 2019 France ... 展开 >> Bordeaux University Hospital Recruiting Bordeaux, France Contact: Chirstophe RICHEZ, MD          Brest University Hospital Recruiting Brest, France Contact: Alain SARAUX, MD          Clermont-Ferrand Hospital Recruiting Clermont-Ferrand, France Contact: Martin SOUBRIER, MDR          Bicêtre Hospital Recruiting Le Kremlin-Bicêtre, France Contact: Xavier MARIETTE, MD          Lille Hospital Recruiting Lille, France Contact: René-Marc FLIPO, MD          Limoges Hospital Recruiting Limoges, France Contact: Pascale Vergne-Salle, MD          Montpellier Hospital Recruiting Montpellier, France Contact: Jacques MOREL, MD          Orléans Hospital Recruiting Orléans, France Contact: Carine SALLIOT, MD          Bichat Hospital Recruiting Paris, France Contact: Philippe DIEUDE, MD          Cochin Hospital Recruiting Paris, France Contact: Yannick Allanore, md          Principal Investigator: Minh Nguyen, MD          La Pitié-Salpétrière Recruiting Paris, France Contact: Laure Gossec, MD          Strasbourg Hospital Recruiting Strasbourg, France Contact: Jacques-Eric Gottenberg, MD          Hospital Pierre-Paul Riquet Recruiting Toujouse, France, 31059 Contact: Adeline RUYSSEN-WITRAND, MD, PhD    05 61 77 56 26 ext 33    ruyssen-witrand.a@chu-toulouse.fr    Contact: Arnaud CONSTANTIN, MD, PhD    05 61 77 69 76 ext 33    constantin.a@chu-toulouse.fr 收起 <<
NCT03421184 Lupus Erythematosus ... 展开 >> Rheumatoid Arthritis Autoimmune Thrombocytopenia 收起 << Not Applicable Recruiting November 2020 France ... 展开 >> CHU de Bordeaux - service de médecine interne Recruiting Pessac, France Contact: Jean-François VIALLARD, Prof    05.57.65.64.83 ext +33    jean-françois.viallard@chu-bordeaux.fr    Contact: Isabelle RAYMOND, Pharm          Principal Investigator: Jean-François VIALLARD, Prof          Sub-Investigator: Estibaliz LAZARO, Prof          Sub-Investigator: Jean-Luc PELLEGRIN, Prof          Sub-Investigator: Carine GREIB, MD          Sub-Investigator: Irene MACHELARD, MD          Sub-Investigator: Marion MIRABEL, MD          Sub-Investigator: Etienne RIVIERE, MD          Sub-Investigator: Thierry SCHAEVERBEKE, Prof          Sub-Investigator: Christophe RICHEZ, Prof          Sub-Investigator: Marie-Elise TRUCHETET, MD          Sub-Investigator: Nicolas POURSAC, MD          Sub-Investigator: Nadia MEHSEN, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.89mL

2.38mL

1.19mL

23.79mL

4.76mL

2.38mL
参考文献

[1]Essayan DM. Cyclic nucleotide phosphodiesterases. J Allergy Clin Immunol. 2001 Nov;108(5):671-80.

[2]Daly JW, Jacobson KA, et al. Adenosine receptors: development of selective agonists and antagonists. Prog Clin Biol Res. 1987;230:41-63.

[3]Glass WF 2nd, Moore JB Jr. Inhibition of human lung cyclic GMP and cyclic AMP phosphodiesterases by certain nucleosides, nucleotides, and pharmacological phosphodiesterase inhibitors. Biochem Pharmacol. 1979 Apr 1;28(7):1107-12. doi: 10.1016/0006-2952(79)90313-7. PMID: 87197.

[4]Maniscalco WM, Wilson CM, Gross I. Influence of aminophylline and cyclic AMP on glycogen metabolism in fetal rat lung in organ culture. Pediatr Res. 1979 Dec;13(12):1319-22. doi: 10.1203/00006450-197912000-00003. PMID: 230447.

[5]Vohra MM. Effect of cyclic AMP, db-cyclic AMP and phosphodiesterase inhibitors on histamine inhibition of the contractile response of the mouse vas deferens. Agents Actions. 1984 Jan;14(1):11-20. doi: 10.1007/BF01966827. PMID: 6199954.

[6]Trembath PW, Shaw J. Potentiation of isoprenaline-induced plasma cyclic AMP response by aminophylline in normal and asthmatic subjects. Br J Clin Pharmacol. 1978 Dec;6(6):499-503. doi: 10.1111/j.1365-2125.1978.tb00873.x. PMID: 215179; PMCID: PMC1429697.