In 1914, Sir Henry Dale provided the basis for the classical and comfortable definition of
muscarinic and nicotinic acetylcholine receptors: Muscarinic receptors are selectively activated …

… ligand giving 50% receptor occupancy (where the free ligand [L]=K d ) is designated EC 50
. Application of the conservation condition for ligand shows directly that EC 50 =K d +[R T ]/2. …

Some antagonists exhibit tissue selectivity in their pharmacological antagonism of
muscarinic responses 1 . However, the affinity constants for equilibrium binding of classical …

The X-ray structure of the photoreceptor rhodopsin has provided the first atomic-resolution
structure of a seven-transmembrane (7-TM) G-protein-coupled receptor. This has provided an …

The interaction of gallamine with muscarinic receptors from different tissues has been
investigated. Gallamine binds to a site distinct from the conventional muscarinic ligand binding site …

The interaction of agonists with muscarinic receptors has been investigated by measuring
the binding of [ 3 H]muscarinic agonists to membrane preparations from the rat cortex and by …

THE C-terminal region of lipotropin, named C fragment 1 , has been found as an intact
polypeptide in the pituitary gland 2 and the C fragment is also released from lipotropin by mild …

Muscarinic acetylcholine receptors (mAChRs) are known to be involved in learning and
memory, but the molecular basis of their involvement is not well understood. The availability of …

The equilibrium binding of muscarinic antagonists to a crude synaptosome fraction from rat
cerebral cortex obeys the simple Langmuir isotherm. The affinity constants measured range …

The crystal structures of antagonist and agonist complexes of isolated β 2 and β 1 adrenoceptors
have recently been supplemented by antagonist structures of M 2 and M 3 muscarinic …