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Chemical Compound Review

SureCN2828700     N-[(1S,4R,6R)-6- bicyclo[2.2.1]heptyl]-9...

Synonyms: AC1L2QMR, N-0861, N 0861, 141696-90-4, N(6)-Endonorbornan-2-yl-9-methyladenine
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Disease relevance of N-0861


High impact information on N-0861


Biological context of N-0861

  • At 60 s postdefibrillation, when other variables were equal, the first derivative of left ventricular pressure in the presence of N-0861 remained 26% greater than placebo [3].
  • RESULTS: There was no change in mean heart rate, arterial and left atrial pressures, +dP/dt, and ultrasonically measured LAD and LCx coronary flows upon N-0861 administration [4].
  • N-0861 alone had only a modest effect on renal or systemic hemodynamics, but produced significant dose-related diuresis/natriuresis [8].
  • The selectivity of antagonism of A1 vs. A2 receptors by N-0861 was evaluated by generating dose-response curves to adenosine-induced bradycardia (A1 effect), and vasodilation in the in situ constant-flow perfused rat hindquarter vasculature (A2 effect) [9].

Anatomical context of N-0861

  • However, in the left atrium, N-0861 (pKB = 6.2) and DPCPX (pKB = 8.9) were no more potent in antagonizing responses to the A1-selective agonists than they were in antagonizing responses to NECA.(ABSTRACT TRUNCATED AT 250 WORDS)[10]
  • Receptor binding studies indicated that N-0861 competitively displaced the binding of 8-cyclopentyl-1,3-[3H]dipropylxanthine to crude guinea pig and human atrial membranes (Ki values of 0.62 and 0.7 microM, respectively) but did not displace the binding of S-(p-nitro[3H]benzyl)-6-thioinosine [11].
  • N-0861 significantly reduced stimulus to His bundle prolongation induced by either hypoxia or reduced perfusion ("ischemia") but did not attenuate the hypoxia-induced decrease in coronary perfusion pressure [11].

Associations of N-0861 with other chemical compounds


Analytical, diagnostic and therapeutic context of N-0861

  • Plasma concentrations of N-0861 were determined with an HPLC method [7].


  1. Selective A2-adenosine receptor agonists do not alter action potential duration, twitch shortening, or cAMP accumulation in guinea pig, rat, or rabbit isolated ventricular myocytes. Shryock, J., Song, Y., Wang, D., Baker, S.P., Olsson, R.A., Belardinelli, L. Circ. Res. (1993) [Pubmed]
  2. Cardiovascular effects of a non-xanthine-selective antagonist of the A1 adenosine receptor in the anaesthetised pig: pharmacological and therapeutic implications. Sidi, A., Wesley, R., Barrett, R., Rush, W., Belardinelli, L. Cardiovasc. Res. (1994) [Pubmed]
  3. Effect of selective A1 adenosine receptor antagonism of postdefibrillation cardiovascular depression: evidence for an antiadrenergic role of endogenous adenosine. Wesley, R.C., Porzio, D., Sadeghi, M. Cardiovasc. Res. (1993) [Pubmed]
  4. Effect of N-0861, a selective adenosine A1 receptor antagonist, on pharmacologic stress imaging with adenosine. Glover, D.K., Ruiz, M., Sansoy, V., Barrett, R.J., Beller, G.A. J. Nucl. Med. (1995) [Pubmed]
  5. Selective attenuation by N-0861 (N6-endonorboran-2-yl-9-methyladenine) of cardiac A1 adenosine receptor-mediated effects in humans. Bertolet, B.D., Belardinelli, L., Franco, E.A., Nichols, W.W., Kerensky, R.A., Hill, J.A. Circulation (1996) [Pubmed]
  6. Inverse agonists and neutral antagonists of recombinant human A1 adenosine receptors stably expressed in Chinese hamster ovary cells. Shryock, J.C., Ozeck, M.J., Belardinelli, L. Mol. Pharmacol. (1998) [Pubmed]
  7. Adenosine A1-receptor occupancy predicts A1-receptor antagonist effects of N-0861. Yasuda, S.U., Nagashima, S., Douyon, E., Benton, R.E., Woosley, R.L., Barbey, J.T. Clin. Pharmacol. Ther. (1998) [Pubmed]
  8. A selective adenosine A1 receptor antagonist attenuates renal dysfunction during controlled hypotension with adenosine in rats. Barrett, R.J., Wright, K.F. Anesth. Analg. (1994) [Pubmed]
  9. N-0861 selectively antagonizes adenosine A1 receptors in vivo. Barrett, R.J., Droppleman, D.A., Wright, K.F. Eur. J. Pharmacol. (1992) [Pubmed]
  10. Identification and functional characterization of A1 and A2 adenosine receptors in the rat vas deferens: a comparison with A1 receptors in guinea pig left atrium and A2 receptors in guinea pig aorta. Martin, P.L., May, J.M. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  11. Evaluation of N-0861, (+-)-N6-endonorbornan-2-yl-9-methyladenine, as an A1 subtype-selective adenosine receptor antagonist in the guinea pig isolated heart. Shryock, J.C., Travagli, H.C., Belardinelli, L. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  12. Adenosine-sensitive afterdepolarizations and triggered activity in guinea pig ventricular myocytes. Song, Y., Thedford, S., Lerman, B.B., Belardinelli, L. Circ. Res. (1992) [Pubmed]
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