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Chemical Compound Review

AC1O5RQN     but-2-enedioic acid; 8-(6-chloropyrazin-2...

Synonyms: L-689660, L-689,660, L 689660
 
 
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Disease relevance of L-689660

  • Centrally-mediated hypothermia was induced by RS86 (0.05 mg/kg p.o.) and L-689,660 (0.01 mg/kg p.o.) but only by a high dose of AF 102B (7 mg/kg p.o.). The putative therapeutic advantages of partial M1/M3 agonists over RS86 are discussed [1].
 

High impact information on L-689660

  • Like 19 and xanomeline, 5i was a functionally selective M1 agonist that showed greater functional selectivity than widely studied pyrazinylquinuclidine 5n (L-689,660) [2].
  • 1-Azabicyclo[2,2,2]octane,3-(6-chloropyrazinyl)maleate (L-689,660) reportedly is an agonist with selectivity for M1 and M3 muscarinic receptors [3].
  • 1. L-689,660, 1-azabicyclo[2.2.2]octane, 3-(6-chloropyrazinyl)maleate, a novel cholinomimetic, demonstrated high affinity binding (pKD (apparent) 7.42) at rat cerebral cortex muscarinic receptors [4].
  • At M1 muscarinic receptors in the rat superior cervical ganglion, L-689,660 was a potent (pEC50 7.3 +/- 0.2) full agonist in comparison with (+/-)-muscarine [4].
  • At M3 receptors in the guinea-pig ileum myenteric plexus-longitudinal muscle or in trachea, L-689,660 was again a potent agonist (pEC50 7.5 +/- 0.2 and 7.7 +/- 0.3 respectively) but had a lower maximum response than carbachol [4].
 

Anatomical context of L-689660

  • L-689,660 had a low ratio (34) of pKD (apparent) values for the displacement of binding of the antagonist ([3H]-N-methylscopolamine ([3H]-NMS) compared with the displacement of the agonist [3H]-oxotremorine-M ([3H]-Oxo-M), in rat cerebral cortex [4].
  • Thus, with functional assays either with brain tissue or with transfected cell lines, L-689,660 was shown to be an agonist for the M1 and M3 receptors but not for M5 or M4 receptors [3].
 

Gene context of L-689660

  • We compare the central and peripheral cholinergic effects of RS86 with the M1/M3 partial agonists AF 102B and L-689,660 ((-)-3-[2-6 chloropyrazin)yl]-1-azabicyclo[2.2.2]octane) in primates [1].

References

  1. Comparison of the effects of selective and nonselective muscarinic agonists on cognition and thermoregulation in primates. Rupniak, N.M., Tye, S.J., Iversen, S.D. J. Neurol. Sci. (1992) [Pubmed]
  2. Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles. Ward, J.S., Merritt, L., Calligaro, D.O., Bymaster, F.P., Shannon, H.E., Sawyer, B.D., Mitch, C.H., Deeter, J.B., Peters, S.C., Sheardown, M.J. J. Med. Chem. (1995) [Pubmed]
  3. Pharmacological characterization of the novel cholinomimetic L-689,660 at cloned and native brain muscarinic receptors. Aagaard, P., McKinney, M. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  4. L-689,660, a novel cholinomimetic with functional selectivity for M1 and M3 muscarinic receptors. Hargreaves, R.J., McKnight, A.T., Scholey, K., Newberry, N.R., Street, L.J., Hutson, P.H., Semark, J.E., Harley, E.A., Patel, S., Freedman, S.B. Br. J. Pharmacol. (1992) [Pubmed]
 
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