PeptideDB

Enprofylline

CAS: 41078-02-8 F: C8H10N4O2 W: 194.19

Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as
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Bioactivity Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease[1][2][3].
Invitro Enprofylline (300 μM) completely blocks the release of IL-8 by N-ethylcarboxamidoadenosine (NECA)[1]. Enprofylline (10 μM) inhibits NECA (10 μM) induced proliferation in a concentration-dependent manner[2]. Cell Proliferation Assay[2] Cell Line:
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:
Name Enprofylline
CAS 41078-02-8
Formula C8H10N4O2
Molar Mass 194.19
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Reference [1]. I Feoktistov, et al. Adenosine A2b receptors evoke interleukin-8 secretion in human mast cells. An enprofylline-sensitive mechanism with implications for asthma. J Clin Invest. 1995 Oct;96(4):1979-86. [2]. M B Grant, et al. Proliferation, migration, and ERK activation in human retinal endothelial cells through A(2B) adenosine receptor stimulation. Invest Ophthalmol Vis Sci. 2001 Aug;42(9):2068-73. [3]. Jiang-Ning Yang, et al. Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed using knockout mice and caffeine. Am J Physiol Heart Circ Physiol. 2009 Apr;296(4):H1141-9.