Results 161 to 170 of about 6,339 (219)
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Characterization of Selective M5 Acetylcholine Muscarinic Receptor Modulators on Dopamine Signaling in the Striatum

The Journal of Pharmacology and Experimental Therapeutics, 2023
The type-5 muscarinic acetylcholine receptor (mAChR, M5) is almost exclusively expressed in dopamine (DA) neurons of the ventral tegmental area and substantia nigra pars compacta; therefore, they are ideally located to modulate DA signaling and underlying behaviors. However, the role of M5 in shaping DA release is still poorly characterized.
Vivien Zell   +12 more
openaire   +2 more sources

Persistent Binding and Functional Antagonism by Xanomeline at the Muscarinic M5 Receptor

The Journal of Pharmacology and Experimental Therapeutics, 2005
Xanomeline is a functionally selective M1/M4 muscarinic acetylcholine receptor agonist. We have previously identified a novel mode of interaction of this ligand with the muscarinic M1 receptor that involves persistent binding and activation of the receptor after extensive washout.
Marianne K O, Grant, Esam E, El-Fakahany
openaire   +2 more sources

Functional expression of rat M5 muscarinic acetylcholine receptor in yeast

Biochemical and Biophysical Research Communications, 1992
We have produced the rat M5 muscarinic acetylcholine receptor, an integral membrane protein, in the yeast Saccharomyces cerevisiae. This was achieved by placing an M5 gene in the yeast vector under the control of the yeast alpha-factor promoter and leader sequence.
Huang, Hao-Jen   +3 more
openaire   +2 more sources

The ontogeny of m1–m5 muscarinic receptor subtypes in rat forebrain

Developmental Brain Research, 1992
The ontogeny of muscarinic receptor subtypes in rat forebrain has been determined utilizing a panel of antisera recognizing unique epitopes of the m1-m5 receptor proteins. Total receptor density in forebrain, as measured by the non-selective antagonist, [3H]quinuclidinyl benzilate (QNB), was found to increase from 507 fmol/mg in neonates (3.5 days) to ...
S J, Wall   +4 more
openaire   +2 more sources

Allosteric regulation of cloned m1–m5 muscarinic receptor subtypes

Biochemical Pharmacology, 1991
Allosteric regulation of [3H]N-methylscopolamine [( 3H]NMS) and [3H]quinuclidinyl benzilate [( 3H]QNB) dissociation from the m1-m5 muscarinic receptor subtypes was examined in transfected CHO-K1 cells. Half-times of dissociation of [3H]NMS from cell membranes (at 23 degrees) ranged from less than 5 min for the m2 subtype to more than 60 min for the m5 ...
J, Ellis, J, Huyler, M R, Brann
openaire   +2 more sources

Linkage of M5 Muscarinic and α7-Nicotinic Receptor Genes on 15q13 to Schizophrenia

Neuropsychobiology, 2004
Most antipsychotic drugs act on the forebrain by blocking dopamine receptors. In rodents, the M5 muscarinic receptor (CHRM5) is important for prolonged dopamine release. We typed polymorphisms in CHRM5 and α7-nicotinic receptor (CHRNA7) genes on 15q13 in 82 Canadian families having at least 1 schizophrenic patient.
De Luca V   +5 more
openaire   +2 more sources

Increased drinking in mutant mice with truncated M5 muscarinic receptor genes

Pharmacology Biochemistry and Behavior, 2002
The rarest and least understood of the muscarinic receptors is the M5 subtype. Recombinant methods were used to create mutant mice with a deletion in the third intracellular loop of the M5 receptor gene. Salivation induced by the nonselective muscarinic agonist pilocarpine (1 mg/kg s.c.) was reduced in homozygous mutants from 15 to 60 min after ...
Junichi, Takeuchi   +9 more
openaire   +2 more sources

Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes

Neuron, 1988
The human and rat genes for a fifth muscarinic receptor have been cloned and expressed in mammalian cells. The 532 amino acid human protein has 89% sequence identity to the 531 amino acid rat protein and is most closely related to the m3 receptor. Both proteins are encoded by single exons.
T I, Bonner   +3 more
openaire   +2 more sources

Development of antisera selective for m4 and m5 muscarinic cholinergic receptors: distribution of m4 and m5 receptors in rat brain.

Molecular Pharmacology, 1993
A portion of the cDNA sequence corresponding to the third intracellular loop of either the m4 or m5 muscarinic cholinergic receptor was ligated into the pRIT23 or pET-3a expression vector, respectively. The expressed fusion proteins were purified and used to develop selective polyclonal antisera to the m4 and m5 muscarinic receptors.
R P, Yasuda   +8 more
openaire   +2 more sources

Intramolecular interactions in muscarinic acetylcholine receptors studied with chimeric m2/m5 receptors.

Molecular Pharmacology, 1994
Current models of the three-dimensional structures of muscarinic acetylcholine receptors and other G protein-coupled receptors are based primarily on high-resolution electron diffraction data obtained with bacteriorhodopsin, the molecular structure of which is characterized by the presence of seven alpha-helical transmembrane domains (TM I-VII ...
Z, Pittel, J, Wess
openaire   +2 more sources

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