title: Pharmacokinetics of 8-phenyltheophylline in the rat.
abstract: The pharmacokinetics of the adenosine antagonist 8-phenyltheophylline (8-PT) have been investigated in the rat. After intravenous administration to male rats with normal renal function, 8-PT was rapidly cleared from plasma with a t1/2 of about 14 min. Its apparent volume of distribution was some 76 mL/100 g and plasma clearance was 3.5 mL min-1/100 g. Injection via the carotid artery did not alter the kinetics of 8-PT, but when given through the portal vein a first-pass effect was observed. Moreover, 8-PT could not be detected in plasma following intraperitoneal injection. The kinetics of 8-PT were not altered in male rats with acute renal failure and no difference was noted between male and female animals with respect to the kinetics of 8-PT following intravenous injection. It is concluded that the pharmacokinetic properties of 8-PT are likely to complicate its use in-vivo.
authors.affiliation: Department of Pharmacology, University of Leeds, UK.
authors.forename: A
authors.initials: A
authors.lastname: Wormald
authors.forename: C J
authors.initials: CJ
authors.lastname: Bowmer
authors.forename: M S
authors.initials: MS
authors.lastname: Yates
authors.forename: M G
authors.initials: MG
authors.lastname: Collis
mesh_terms: D058186:Acute Kidney Injury / Q000188:drug therapy / Q000378:metabolism; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D007269:Injections, Intra-Arterial; D007275:Injections, Intravenous; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013806:Theophylline / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
chemical_list: D013806:Theophylline; C028322:8-phenyltheophylline