Chemical Properties
White Solid
Uses
A metabolite of Theophylline in human plasma.
Definition
ChEBI: Proxyphylline is an oxopurine.
Biological Activity
ki: 82 nm for bovine brain a1 adenosine receptorproxyphylline is an a1 adenosine receptor antagonist.the a1 adenosine receptor, the best characterized purinergic receptor family, can mediate responses via multiple pertussis toxin-sensitive gtp binding proteins to various different effectors.
in vitro
previous study showed that proxyphylline could selectively antagonize a1 adenosine receptors versus a2 adenosine receptors (ki = 850 μm for platelets) [1].
in vivo
in a previous study, rats that were allodynic following the vincristine injections were randomly allocated into four groups. theoesberiven f (a combination of proxyphylline and melilotus extract) was administered to rats. results showed that the decreased paw withdrawal threshold induced by vincristine injection was increased by theoesberiven f treatment and the increased withdrawal frequency to cold stimuli was also reduced by theoesberiven f treatment [2].
Purification Methods
Crystallise it from EtOH, aqueous MeOH or EtOAc. Roth Archiv Pharmazie 292 234 1959, Zelnik et al. Bull Soc Chim Fr 1733 1956, Beilstein 26 III/IV 2366.]
References
[1] u. schwabe, d. ukena and m. j. lohse. xanthine derivatives as antagonists at a1 and a2 adenosine receptors. naunyn-schmiedeberg's arch.pharmacol. 330,212-221 (1985).
[2] s. bang, y. s. kim and s. r. jeong. anti-allodynic effect of theoesberiven f in a vincristine-induced neuropathy model. exp. ther. med. 12(2), 799-803 (2016).
[3] selvig k. pharmacokinetics of proxyphylline in adults after intravenous and oral administration. eur j clin pharmacol. 1981 jan;19(2):149-55.
