title: L-687,306: a functionally selective and potent muscarinic M1 receptor agonist.
abstract: 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.
authors.affiliation: Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK.
authors.forename: S B
authors.initials: SB
authors.lastname: Freedman
authors.forename: S
authors.initials: S
authors.lastname: Patel
authors.forename: E A
authors.initials: EA
authors.lastname: Harley
authors.forename: L L
authors.initials: LL
authors.lastname: Iversen
authors.forename: R
authors.initials: R
authors.lastname: Baker
authors.forename: G A
authors.initials: GA
authors.lastname: Showell
authors.forename: J
authors.initials: J
authors.lastname: Saunders
authors.forename: A
authors.initials: A
authors.lastname: McKnight
authors.forename: N
authors.initials: N
authors.lastname: Newberry
authors.forename: K
authors.initials: K
authors.lastname: Scholey
mesh_terms: D000818:Animals; D001643:Bridged Bicyclo Compounds / Q000494:pharmacology*; D019086:Bridged Bicyclo Compounds, Heterocyclic; D005727:Ganglia, Spinal / Q000187:drug effects / Q000502:physiology / Q000648:ultrastructure; D006168:Guinea Pigs; D009116:Muscarine / Q000494:pharmacology; D009197:Myenteric Plexus / Q000187:drug effects / Q000502:physiology; D009469:Neuromuscular Junction / Q000187:drug effects / Q000502:physiology; D010069:Oxadiazoles / Q000494:pharmacology*; D051381:Rats; D011976:Receptors, Muscarinic / Q000502:physiology*
chemical_list: D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D010069:Oxadiazoles; D011976:Receptors, Muscarinic; C067804:L 670548; C076510:L 687306; D009116:Muscarine