L-687,306: a functionally selective and potent muscarinic M1 receptor agonist
| Autor: | Leslie L. Iversen, Raymond Baker, A.T. McKnight, John Saunders, Kate Scholey, Richard Hargreaves, Nigel R. Newberry, Stephen B. Freedman, Graham Andrew Showell, Shil Patel, E.A. Harley |
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| Rok vydání: | 1992 |
| Předmět: |
Agonist
medicine.medical_specialty medicine.drug_class Guinea Pigs Neuromuscular Junction Myenteric Plexus Biology Muscarinic agonist Partial agonist Bridged Bicyclo Compounds Ganglia Spinal Muscarine Internal medicine medicine Muscarinic acetylcholine receptor M4 Animals Inverse agonist Pharmacology Oxadiazoles Muscarinic acetylcholine receptor M3 Muscarinic acetylcholine receptor M2 Muscarinic acetylcholine receptor M1 Bridged Bicyclo Compounds Heterocyclic Receptors Muscarinic Rats Endocrinology |
| Zdroj: | European Journal of Pharmacology. 215:135-136 |
| ISSN: | 0014-2999 |
| DOI: | 10.1016/0014-2999(92)90618-e |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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