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Chemical Compound Review

FT-0664498     sodium3-[4-[2-[[6-amino-9- [(2R,3R,4S,5S)...

Synonyms: AC1MJ6GT, 120225-64-1
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Disease relevance of CGS21680


High impact information on CGS21680


Biological context of CGS21680

  • Furthermore, blockade of the beta adrenergic receptor with metoprolol (1 mg/kg, i.v.) significantly attenuated the increase in heart rate produced by NECA, CGS 21680C and CGS 24012 [7].
  • Both compounds were considerably less active at A1 receptors with CGS 21577 and CGS 21680C having respective IC50 values of 0.76 and 3.1 microM [8].
  • Hindquarter, renal and mesenteric vascular resistances were significantly reduced by both CGS 21680C and CGS 24012, whereas only mesenteric vascular resistance was reduced with NECA [7].
  • At equihypotensive doses, both CGS 21680C and CGS 24012 produced significant increases in cardiac output, but NECA had no effect [7].
  • Effects of a putative A2-adenosine receptor agonist 2-[(p-2-carboxyethyl)-phenethylamino]-5'-N-ethyl-carboxamide-adeno sine (CGS 21680C) on force of contraction, protein phosphorylation, cyclic adenosine monophosphate (cAMP) content, and the activity of phosphodiesterase (PDE) isoenzymes in guinea pig ventricular (GPV) preparations were studied [9].

Anatomical context of CGS21680


Associations of CGS21680 with other chemical compounds


Gene context of CGS21680


  1. Stimulation of adenosine A2a receptors in the rat striatum induces catalepsy that is reversed by antagonists of N-methyl-D-aspartate receptors. Hauber, W., Münkle, M. Neurosci. Lett. (1995) [Pubmed]
  2. Cardiovascular responses to adenosine in fetal sheep: autonomic blockade. Koos, B.J., Mason, B.A., Ducsay, C.A. Am. J. Physiol. (1993) [Pubmed]
  3. Quantification of the in vivo potency of the adenosine A2 receptor antagonist 8-(3-chlorostyryl)caffeine. Mathôt, R.A., Gubbens-Stibbe, J.M., Soudijn, W., Jacobson, K.A., Ijzerman, A.P., Danhof, M. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  4. Potentiation by tonic A2a-adenosine receptor activation of CGRP-facilitated [3H]-ACh release from rat motor nerve endings. Correia-de-Sá, P., Ribeiro, J.A. Br. J. Pharmacol. (1994) [Pubmed]
  5. Development of tolerance to the antihypertensive effects of highly selective adenosine A2a agonists upon chronic administration. Webb, R.L., Sills, M.A., Chovan, J.P., Peppard, J.V., Francis, J.E. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  6. Role of endothelium-derived relaxing factor in the in vivo renal vascular action of adenosine in dogs. Okumura, M., Miura, K., Yamashita, Y., Yukimura, T., Yamamoto, K. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  7. Cardiovascular effects of adenosine A2 agonists in the conscious spontaneously hypertensive rat: a comparative study of three structurally distinct ligands. Webb, R.L., Barclay, B.W., Graybill, S.C. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  8. CGS 21680C, an A2 selective adenosine receptor agonist with preferential hypotensive activity. Hutchison, A.J., Webb, R.L., Oei, H.H., Ghai, G.R., Zimmerman, M.B., Williams, M. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  9. Characterization of biochemical effects of CGS 21680C, an A2-adenosine receptor agonist, in the mammalian ventricle. Bokník, P., Neumann, J., Schmitz, W., Scholz, H., Wenzlaff, H. J. Cardiovasc. Pharmacol. (1997) [Pubmed]
  10. Adenosine inhibits leukocyte-induced vasoconstriction. Minamino, T., Kitakaze, M., Node, K., Funaya, H., Inoue, M., Hori, M., Kamada, T. Am. J. Physiol. (1996) [Pubmed]
  11. Adenosine-induced vasodilation: receptor characterization in pulmonary circulation. Haynes, J., Obiako, B., Thompson, W.J., Downey, J. Am. J. Physiol. (1995) [Pubmed]
  12. Tonic adenosine A2A receptor activation modulates nicotinic autoreceptor function at the rat neuromuscular junction. Correia-de-Sá, P., Ribeiro, J.A. Eur. J. Pharmacol. (1994) [Pubmed]
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