L-687,306: a functionally selective and potent muscarinic M1 receptor agonist.
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.
Freedman
S B
SB
Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, UK.
Patel
S
S
Harley
E A
EA
Iversen
L L
LL
Baker
R
R
Showell
G A
GA
Saunders
J
J
McKnight
A
A
Newberry
N
N
Scholey
K
K
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*
D001643:Bridged Bicyclo Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D010069:Oxadiazoles; D011976:Receptors, Muscarinic; C067804:L 670548; C076510:L 687306; D009116:Muscarine