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Allosteric Modulators: The New Generation of Receptor Antagonist
Table 1.
Selectivity of Agonists and Allosteric Antagonists for Muscarinic Receptor Subtypes: pK A 1 or pK B 2 values
| M1 | M2 | M3 | M4 | Range3 | |
|---|---|---|---|---|---|
| 1 pK A = - log equilibrium dissociation constants for agonists acetylcholine, oxotremorine, carbachol, pilocarpine, and bethanechol for muscarinic receptor subtypes. | |||||
| 2 pK B = - log equilibrium dissociation constants for antagonists alcuronium, strychnine, brucine, vincamine, and eburnamonine for muscarinic receptor subtypes. | |||||
| 3 Range refers to the multiple maximal difference between the affinities (i.e., K A or K B values) of the ligands for the muscarinic receptor subtypes. Data from (3). | |||||
| Acetylcholine | 4.3 | 4.3 | 4.5 | 4.5 | 1.6 |
| Oxotremorine | 5.5 | 5 | 5.3 | 5.2 | 3.2 |
| Carbachol | 4.5 | 4.2 | 4.4 | 4.3 | 1.6 |
| Pilocarpine | 5.1 | 4.9 | 5.1 | 5.2 | 2.0 |
| Bethanechol | 4 | 4.1 | 4.1 | 4 | 1.3 |
| Alcuronium | 5 | 6.1 | 5.8 | 5.6 | 12.6 |
| Strychnine | 5 | 4.9 | 5.7 | 4.8 | 7.9 |
| Brucine | 5.7 | 4.6 | 4 | 6 | 100 |
| Vincamine | 4.8 | 5.1 | 5.7 | 4.2 | 31.6 |
| Eburnamonine | 5.1 | 4.2 | 5.2 | 4.6 | 10 |
