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L-687,306: a functionally selective and potent muscarinic M1 receptor agonist. 1992
S B Freedman, and
S Patel, and
E A Harley, and
L L Iversen, and
R Baker, and
G A Showell, and
J Saunders, and
A McKnight, and
N Newberry, and
K Scholey
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK.
The oxadiazole L-687,306 is a high affinity muscarinic agonist with a N-methylscopolamine/oxotremorine-M binding profile predictive of a partial agonist. L-687,306 showed marked selectivity in functional pharmacological assays. L-687,306 was a partial agonist at muscarinic M1 receptors in the rat ganglion but a high affinity competitive antagonist at guinea-pig cardiac M2 and ileal M3 muscarinic receptors. This compound gives an opportunity to study receptor reserve involved in muscarinic receptors in vitro and in vivo.
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