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] BRUNS R F. Adenosine antagonism by purines, pteridines and benzopteridines in human fibroblasts[J]. Biochemical pharmacology, 1981, 30 4: Pages 325-333. DOI:
10.1016/0006-2952(81)90062-9[2] KEISUKE TAKEDA . EFFECTS OF AMINOPHYLLINE, PROXYPHYLLINE AND A PROXYPHYLINE-MELILOTUS EXTRACT-RUTIN MIXTURE (THEOESBERIVEN) ON THE HEART AND THE CORONARY CIRCULATION[J]. Japanese journal of pharmacology, 1977, 27 5: Pages 709-720. DOI:
10.1254/jjp.27.709[3] LUCYNA KORZYCKA Dorota G. Synthesis, pharmacological activity and nitric oxide generation by nitrate derivatives of theophylline.[J]. Journal of Pharmacy and Pharmacology, 2008, 60 5: 637-645. DOI:
10.1211/jpp.60.5.0010[4] KNUT DALAKER Hans P. Effect of some drugs on thromboplastin activity in mouse trophoblast cells in vitro and in vivo[J]. Biochemical pharmacology, 1986, 35 20: Pages 3433-3439. DOI:
10.1016/0006-2952(86)90609-x
