Radioligand binding characteristics of the chicken cardiac muscarinic receptor

1989 ◽  
Vol 340 (3) ◽  
Author(s):  
AntonD. Michel ◽  
RogerL. Whiting
Keyword(s):  
Muscarinic Receptor ◽  
Radioligand Binding ◽  
Binding Characteristics

scholarly journals Radioligand Binding Characteristics of the Endothelin Receptor in the Rabbit Iris

1998 ◽  
Vol 76 (3) ◽  
pp. 289-296 ◽  
Author(s):  
Chihiro Nosaka ◽  
Hitoshi Ishikawa ◽  
Isao Haruno ◽  
Takeshi Yoshitomi ◽  
Hiroshi Kase ◽  
...  
Keyword(s):  
Radioligand Binding ◽  
Endothelin Receptor ◽  
Binding Characteristics ◽  
Rabbit Iris

Neuromuscular Relaxants as Antagonists for M2and M3Muscarinic Receptors 

1998 ◽  
Vol 88 (3) ◽  
pp. 744-750 ◽  
Author(s):  
Vivian Y. Hou ◽  
Carol A. Hirshman ◽  
Charles W. Emala
Keyword(s):  
Muscarinic Receptor ◽  
Muscarinic Receptors ◽  
Radioligand Binding ◽  
Chinese Hamster ◽  
Neuromuscular Relaxants ◽  
Ovary Cell ◽  
Relative Order ◽  
Parasympathetic Nerves ◽  
M2 Muscarinic Receptor ◽  
M3 Muscarinic Receptor

Background Neuromuscular relaxants such as pancuronium bind to M2 and M3 muscarinic receptors as antagonists. Blockade of muscarinic receptors in atria of the M2 subtype mediates tachycardia. In the lung, blockade of M2 receptors on parasympathetic nerves potentiates vagally induced bronchospasm, whereas blockade of M3 receptors on bronchial smooth muscle inhibits bronchospasm. The current study was designed to quantify the affinity of a series of neuromuscular relaxants for the M2 and M3 muscarinic receptors, which were individually stably transfected in Chinese hamster ovary cell lines. Methods Competitive radioligand binding assays determined the relative binding affinities of the neuromuscular relaxants pancuronium, succinylcholine, mivacurium, doxacurium, atracurium, rocuronium, gallamine, and pipecuronium for the muscarinic receptor in the presence of a muscarinic receptor antagonist (3H-QNB) in membranes prepared from cells individually expressing either the M2 or M3 muscarinic receptor. Results All muscle relaxants evaluated displaced 3H-QNB from muscarinic receptors. The relative order of potency for the M2 muscarinic receptor (highest to lowest) was pancuronium, gallamine, rocuronium, atracurium, pipecuronium, doxacurium, mivacurium, and succinylcholine. The relative order of potency for the M3 muscarinic receptor (highest to lowest) was pancuronium, atracurium, pipecuronium, rocuronium, mivacurium, gallamine, succinylcholine, and doxacurium. Conclusions All neuromuscular relaxants studied had affinities for the M2 and M3 muscarinic receptor, but only pancuronium and gallamine had affinities within the range of concentrations achieved with clinical use. The high affinities of gallamine and pancuronium for the M2 muscarinic receptor are consistent with a mechanism of M2 receptor blockade in relaxant-induced tachycardia.

Human Muscarinic Receptor Binding Characteristics of Antimuscarinic Agents to Treat Overactive Bladder

2006 ◽  
Vol 175 (1) ◽  
pp. 365???369
Author(s):  
Shuji Maruyama ◽  
Tomomi Oki ◽  
Atsushi Otsuka ◽  
Hitoshi Shinbo ◽  
Seiichiro Ozono ◽  
...  
Keyword(s):  
Overactive Bladder ◽  
Muscarinic Receptor ◽  
Receptor Binding ◽  
Antimuscarinic Agents ◽  
Binding Characteristics

Binding Characteristics of the Muscarinic Receptor Subtype in Rabbit Pancreas

1990 ◽  
Vol 10 (1-2) ◽  
pp. 119-135 ◽  
Author(s):  
A. J. G. Van Zwam ◽  
P. H.G.M. Willems ◽  
J. F. Rodrigues De Miranda ◽  
J. J.H.H.M. De Pont ◽  
C. A.M. Van Ginneken
Keyword(s):  
Muscarinic Receptor ◽  
Receptor Subtype ◽  
Muscarinic Receptor Subtype ◽  
Binding Characteristics ◽  
Rabbit Pancreas

A high-affinity folate binding protein in human urine. Radioligand binding characteristics, immunological properties and molecular size

1989 ◽  
Vol 9 (1) ◽  
pp. 93-97 ◽  
Author(s):  
Steen Ingemann Hansen ◽  
Jan Holm ◽  
Mimi Høier-Madsen
Keyword(s):  
Human Urine ◽  
Radioligand Binding ◽  
Binding Protein ◽  
Molecular Size ◽  
Enzyme Linked Immunosorbent Assay ◽  
Folate Binding Protein ◽  
Binding Characteristics ◽  
High Affinity ◽  
Large Peak ◽  
Apparently Healthy

High-affinity binding of [3H]folate in human urine displayed characteristics, e.g. apparent positive cooperativity, which are typical of specific folate binding. By means of a two-site enzyme-linked immunosorbent assay (ELISA) with rabbit antibodies against the low molecular weight folate binding protein from human milk, we measured folate binding protein concentrations in the range of 0.51 to 4.13 nM in urine samples from 16 apparently healthy individuals. Ultrogel AcA 44 chromatography of the urine showed that immunoreactive and radioligand bound folate binding protein coeluted in one large peak (Mr∼25,000).

Characterization of a muscarinic receptor controlling Cl- secretion in hen trachea

1990 ◽  
Vol 258 (6) ◽  
pp. C982-C987 ◽  
Author(s):  
B. Winding ◽  
N. Bindslev
Keyword(s):  
Muscarinic Receptor ◽  
Muscarinic Receptors ◽  
Radioligand Binding ◽  
Receptor Subtype ◽  
Coupling Mechanism ◽  
Serosal Side ◽  
Functional Responses ◽  
Binding Studies ◽  
Muscarinic Receptor Subtype ◽  
Cl Secretion

We have attempted to characterize a muscarinic receptor subtype involved in Cl- secretion in isolated epithelium of hen trachea, taking advantage of drugs developed in the last 15 yr. Hen trachea can be stimulated to secrete Cl- equal to approximately 80-90 microA/cm2 by application of acetylcholine (ACh) to the serosal side. The process has an apparent dissociation constant (Kd) for ACh of 740 nM. The Cl- secretion is completely inhibited by 20 microM bumetanide at the serosal side. Of five selective antagonists for muscarinic receptors, pirenzepine, hexahydrosiladifenidol, dicyclomine, 11-([2-[(diethylamino)-methyl]-1-piperidinyl]acetyl)-5,11- dihydro-6H-pyrido(2,3-b)(1,4)benzodiazepine-6-one, and 4 diphenyl acetoxy-N-methylpiperidine methobromide, only the latter had a high affinity for the functional receptor with an apparent Kd of 3 nM. The receptor may be classified as an M4-muscarinic receptor subtype and probably belongs to a group of muscarinic receptors on exocrine glands and mucosal cells involved in ion transport. All the functional responses caused by muscarinic agonists and antagonists tested exhibited exponents (apparent Hill coefficients) in the range from 1.3 to 2.4, indicating a gain in the stimulus secretion coupling mechanism, an aspect of muscarinic receptor function that is not revealed in radioligand binding studies.

scholarly journals Muscarinic receptor subtypes in human bladder detrusor and mucosa, studied by radioligand binding and quantitative competitive RT-PCR: changes in ageing

2005 ◽  
Vol 144 (8) ◽  
pp. 1089-1099 ◽  
Author(s):  
Kylie J Mansfield ◽  
Lu Liu ◽  
Frederick J Mitchelson ◽  
Kate H Moore ◽  
Richard J Millard ◽  
...  
Keyword(s):  
Muscarinic Receptor ◽  
Radioligand Binding ◽  
Receptor Subtypes ◽  
Muscarinic Receptor Subtypes ◽  
Rt Pcr ◽  
Human Bladder ◽  
Bladder Detrusor

scholarly journals Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Frank Herrmann ◽  
Manuela Hessmann ◽  
Sabine Schaertl ◽  
Karola Berg-Rosseburg ◽  
Christopher J Brown ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Trinucleotide Repeat ◽  
Radioligand Binding ◽  
Ex Vivo ◽  
Binding Assays ◽  
Pharmacological Characterization ◽  
Binding Characteristics

AbstractHuntington’s disease (HD) is caused by a CAG trinucleotide repeat expansion in the first exon of the huntingtin (HTT) gene coding for the huntingtin (HTT) protein. The misfolding and consequential aggregation of CAG-expanded mutant HTT (mHTT) underpin HD pathology. Our interest in the life cycle of HTT led us to consider the development of high-affinity small-molecule binders of HTT oligomerized/amyloid-containing species that could serve as either cellular and in vivo imaging tools or potential therapeutic agents. We recently reported the development of PET tracers CHDI-180 and CHDI-626 as suitable for imaging mHTT aggregates, and here we present an in-depth pharmacological investigation of their binding characteristics. We have implemented an array of in vitro and ex vivo radiometric binding assays using recombinant HTT, brain homogenate-derived HTT aggregates, and brain sections from mouse HD models and humans post-mortem to investigate binding affinities and selectivity against other pathological proteins from indications such as Alzheimer’s disease and spinocerebellar ataxia 1. Radioligand binding assays and autoradiography studies using brain homogenates and tissue sections from HD mouse models showed that CHDI-180 and CHDI-626 specifically bind mHTT aggregates that accumulate with age and disease progression. Finally, we characterized CHDI-180 and CHDI-626 regarding their off-target selectivity and binding affinity to beta amyloid plaques in brain sections and homogenates from Alzheimer’s disease patients.

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