1989
DOI: 10.1111/j.1476-5381.1989.tb11802.x
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1,3,8‐ and 1,3,7‐substituted xanthines: relative potency as adenosine receptor antagonists at the frog neuromuscular junction

Abstract: 1 The ability of 1,3,8-substituted xanthines (1,3-dipropyl-8-(4(2-aminoethyl)amino) carbonylmethyloxyphenyl)xanthine (XAC), 1,3-dipropyl-8(4-carboxymethyloxyphenyl)xanthine (XCC), 1,3-dipropyl-8-2-amino-4-chlorophenyl)xanthine (PACPX), 1,3-dipropyl-8-cyclopentylxanthine (DPCPX), 1,3-diethyl-8-phenylxanthine (DPX) and 8-phenyltheophylline (8-PT)), of 1,3,7-substituted xanthines (1-propargyl-3,7-dimethylxanthine (PGDMX) and caffeine), and of a 3-substituted xanthine (enprofylline) to antagonize the inhibitory… Show more

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Cited by 37 publications
(16 citation statements)
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“…This agrees with the idea that the adenosine receptor mediating inhibition of neurotransmitter release is not coupled to adenylate cyclase (see e.g. Ribeiro & Sebastiao, 1989).…”
Section: Discussionsupporting
confidence: 92%
See 1 more Smart Citation
“…This agrees with the idea that the adenosine receptor mediating inhibition of neurotransmitter release is not coupled to adenylate cyclase (see e.g. Ribeiro & Sebastiao, 1989).…”
Section: Discussionsupporting
confidence: 92%
“…amplitude caused by 0.5 pg ml 1, lugml-' and 2.5pgml-1 of polymyxin B were 8 + 1.0% (n = 2), 19 + 1.4% (n = 6) and 31 + 2.0% (n = 2) respectively. The quantal content (determined by the variance method) of Ribeiro, 1989). Ki values were taken as the negative antilog of the pA2 value.…”
Section: H-7 and Polymyxin Bmentioning
confidence: 99%
“…The rank order of potency of antagonists found was: 8-phenyltheophylline>xanthine amino congener (XAC)= DPCPX = CGS15943>isobutyl methylxanthine (IBMX) > > theophylline. The similar potency of XAC and DPCPX can be compared to that corresponding to A3 receptors, although the Ki values obtained with BBM in our displacement experiments are higher than those reported from functional studies for the A3 receptor (Sebastiao & Ribeiro, 1989). What is still evident is that the order for antagonists does not coincide with those which are well established for Al (DPCPX> xanthine amino congener> theophylline) and A2 (CGS15943>xanthine amino con-gener> DPCPX> theophylline) receptors.…”
Section: Discussioncontrasting
confidence: 48%
“…Metabolism was monitored at the end of incubation period (see Figure 1); at this time more than 18% of added AP4A and more than 55% of added AP5A was not metabolized. As shown in Table 3 Pertussis toxin (pg ml1) (Sebastiao & Ribeiro, 1989). What is still evident is that the order for antagonists does not coincide with those which are well established for Al (DPCPX> xanthine amino congener> theophylline) and A2 (CGS15943>xanthine amino congener> DPCPX> theophylline) receptors.…”
Section: Discussionmentioning
confidence: 90%
“… a Bruns et al, 1987; b Haleen et al, 1987; c Lee and Reddington, 1986; d Jacobson et al, 1993 a ; e Bruns et al, 1986; f Ukena et al, 1986; g Choi et al, 1988; h Seale et al, 1988; i Sebastiao and Ribeiro, 1989; j Jacobson et al, 1993 b . …”
Section: Effects Of Adenosine Antagonists On Neca‐induced Cis‐cos Myomentioning
confidence: 99%