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Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
The discovery that it is possible to increase the affinity of muscarinic receptors for their agonists by allosteric modulators offers a new way to subtype-specific pharmacological enhancement of transmission at cholinergic (muscarinic) synapses. Expand
An arginine residue conserved in most G protein-coupled receptors is essential for the function of the m1 muscarinic receptor.
Data demonstrate for the first time that this highly conserved arginine residue plays an important role in coupling of muscarinic receptors to signal transduction mechanisms. Expand
The assessment of antagonist potency under conditions of transient response kinetics.
The muscarinic acetylcholine receptor antagonists, atropine and pirenzepine, produced an apparent insurmountable antagonism of muscarinic M(1) receptor-mediated intracellular Ca(2+) mobilization inExpand
Marked Induction of Calcium-Independent Nitric Oxide Synthase Activity after Focal Cerebral Ischemia
The results suggest that the decline in calcium-dependent (cNOS) activity reflects loss of NOS neurons within the lesion, and sustained nitric oxide production by iNOS may contribute to the late phase of tissue damage in focal cerebral ischemia. Expand
NMDA Receptor-Mediated Refinement of a Transient Retinotectal Projection during Development Requires Nitric Oxide
NMDA receptor-mediated elimination of the ipsilateral retinotectal projection is completely mediated via nitric oxide, suggesting that NMDA receptor activation can regulateNitric oxide synthase activity in the tectum. Expand
Polyamines inhibit nitric oxide synthase in rat cerebellum
Evidence was obtained, however, that endogenous polyamines are not involved in regulation of NMDA-stimulated NO synthase activity, and the observed inhibitory effects of exogenous polyamines might not reflect a physiological role in modulating NO generation in neurons. Expand
Constitutive activity of the M1–M4 subtypes of muscarinic receptors in transfected CHO cells and of muscarinic receptors in the heart cells revealed by negative antagonists
It is concluded that the M1–M4 subtypes of muscarinic receptors are constitutively active in the CHO cell lines expressing them and in cardiomyocytes and that atropine and NMS act as negative antagonists on these receptor subtypes by stabilizing them in the inactive conformation. Expand
Muscarinic M2 Receptors Directly Activate Gq/11 and Gs G-Proteins
Direct evidence of M2 receptor coupling with the α subunits of Gs and Gq/11 G-proteins is provided and induction of multiple receptor conformational states dependent on both the concentration and the nature of the agonist used is demonstrated. Expand
The Role of Nitric Oxide in Development of Topographic Precision in the Retinotectal Projection of Chick
The results show that nitric oxide is involved in refinement of the topography of the retinotectal projection as well as in other aspects of refinement of this projection in developing chick. Expand
Evidence for a Tandem Two-site Model of Ligand Binding to Muscarinic Acetylcholine Receptors*
Experimental data on [ 3H]NMS and [3H]QNB association and dissociation perfectly agree with the predictions of the tandem two-site model, which support a model in which the receptor binding domain has two tandemly arranged subsites for classical ligands, a peripheral one and a central one. Expand