| Identification | Back Directory | [Name]
ENPROFYLLINE | [CAS]
41078-02-8 | [Synonyms]
d-4028
nilyph
Enprofilina
ENPROFYLLINE
Enprofyllinum
Enprofyllilie
ENPROPHYLLINE
3-PROPYLXANTHINE
3-Propylxanthfine
3-N-PROPYLXANTHINE
3-propyl-7H-purine-2,6-dione
3-propyl-7H-purine-2,6-quinone
3-Propyl-1H-purine-2,6(3H,7H)-dione
3-Propyl-7H-purine-2,6(1H,3H)-dione
3,9-dihydro-3-propyl-purine-2,6-dione
3,7-dihydro-3-propyl-1h-purine-6-dione
3,7-dihydro-3-propyl-1h-purine-2,6-dione
3-Propyl 3,7-dihydro-1H-purine-2,6-dione
1H-Purine-2,6-dione, 3,9-dihydro-3-propyl-
3-propyl-2,3,6,7-tetrahydro-1H-purin-2,6-dione
chronic obstructive pulmonary,interleukin-8,A2B receptor antagonist,phosphodiesterase inhibitor,Enprofylline,Adenosine Receptor,Adenosine,inhibit,asthma,Inhibitor,phospholipase C,P1 receptor,Phosphodiesterase (PDE) | [EINECS(EC#)]
255-201-8 | [Molecular Formula]
C8H10N4O2 | [MDL Number]
MFCD00043205 | [MOL File]
41078-02-8.mol | [Molecular Weight]
194.19 |
| Hazard Information | Back Directory | [Description]
3-Propylxanthine is a xanthine derivative that antagonizes adenosine receptors (Kis = 44, 32, and 6.3 μM for A1, A2A, and A2B, respectively) and cAMP phosphodiesterase (Ki = 42 μM). Through these actions, 3-propylxanthine induces smooth muscle relaxation, blocks smooth muscle contraction and VEGF secretion driven by adenosine receptor agonists, and reduces bronchial hyperresponsiveness. | [Uses]
Bronchodilator. | [Definition]
ChEBI: Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic n
uropathy. | [in vivo]
Enprofylline increases heart rate (HR). Injection of Enprofylline (7.5 and 30 mg/kg) increases HR in male WT mouse from 529±23 to 590±20 and 562±20 after the low and high dose, respectively[3].
A high dose of Enprofylline (30 mg/kg) also decreases temperature compared with saline injection in female (but not in males) WT mice, but a low dose (7.5 mg/kg) has little effect on mouse temperature[3]. | Animal Model: | A1RKO mice (were cross-bred to C57BL/6 mice for six generations) and A2ARKO mice (were backcrossed to C57BL/6 mice for more than 10 generations)[3] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneally injected (bolus) at 2-h intervals | | Result: | Increased HR in male WT mouse from 529±23 to 590±20 and 562±20 after the low (7.5 mg/kg) and high dose (30 mg/kg), respectively. |
| [IC 50]
A2B receptor: 7 μM (Ki) | [storage]
Store at -20°C | [References]
[1] J LINDEN. Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.[J]. Molecular Pharmacology, 1999, 56 4: 705-713.
[2] K. OGAWA T. S K Takagi. Mechanism of xanthine-induced relaxation of guinea-pig isolated trachealis muscle[J]. British Journal of Pharmacology, 1989, 97 2: 542-546. DOI: 10.1111/j.1476-5381.1989.tb11983.x
[3] U SCHWABE M J L D Ukena. Xanthine derivatives as antagonists at A1 and A2 adenosine receptors.[J]. Naunyn-Schmiedeberg’s archives of pharmacology, 1985, 330 3: 212-221. DOI: 10.1007/bf00572436
[4] BIRGITTE H?IER. Contraction-induced secretion of VEGF from skeletal muscle cells is mediated by adenosine.[J]. American journal of physiology. Heart and circulatory physiology, 2010: H857-62. DOI: 10.1152/ajpheart.00082.2010
[5] G H KO?TER. Effect of theophylline and enprofylline on bronchial hyperresponsiveness.[J]. Thorax, 1989, 44 12: 1022-1026. DOI: 10.1136/thx.44.12.1022 |
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| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
|