Acute treatment with pentobarbital alters the kinetics of in vivo receptor binding in the mouse brain

2006 ◽  
Vol 33 (4) ◽  
pp. 535-541 ◽  
Author(s):  
Yojiro Sakiyama ◽  
Masao Saito ◽  
Osamu Inoue
Keyword(s):  
Mouse Brain ◽  
Receptor Binding ◽  
Acute Treatment ◽  
Kinetics Of ◽  
In Vivo Receptor Binding

Difference in in vivo receptor binding between [3 H]N-methylspiperone and [3 H]raclopride in reserpine-treated mouse brain

1991 ◽  
Vol 85 (1) ◽  
pp. 1-10 ◽  
Author(s):  
O. Inoue ◽  
K. Kobayashi ◽  
H. Tsukada ◽  
T. Itoh ◽  
B. Langstrom
Keyword(s):  
Mouse Brain ◽  
Receptor Binding ◽  
Treated Mouse ◽  
In Vivo Receptor Binding

In vitro and in vivo receptor binding and deoxyglucose studies in rat brain with the potential antipsychotic Org 5222

1990 ◽  
Vol 183 (5) ◽  
pp. 1623
Author(s):  
J.A.D.M. Tonnaer ◽  
P. Room ◽  
W.M.J.B. Van Gemert ◽  
L.P.C. Delbressine ◽  
T. de Boer ◽  
...  
Keyword(s):  
Rat Brain ◽  
Receptor Binding ◽  
In Vivo Receptor Binding

scholarly journals Ligand-receptor binding kinetics in drug design

2020 ◽  
Vol 66 (1) ◽  
pp. 42-53
Author(s):  
D.V. Borisov ◽  
A.V. Veselovsky
Keyword(s):  
Ligand Binding ◽  
Receptor Binding ◽  
Rational Design ◽  
Drug Binding ◽  
New Drugs ◽  
Receptor Ligand ◽  
Molecular Features ◽  
Kinetics Of

Traditionally, the thermodynamic values of affinity are considered as the main criterion for the development of new drugs. Usually, these values for drugs are measured in vitro at steady concentrations of the receptor and ligand, which are differed from in vivo environment. Recent studies have shown that the kinetics of the process of drug binding to its receptor make significant contribution in the drug effectiveness. This has increased attention in characterizing and predicting the rate constants of association and dissociation of the receptor ligand at the stage of preclinical studies of drug candidates. A drug with a long residence time can determine ligand-receptor selectivity (kinetic selectivity), maintain pharmacological activity of the drug at its low concentration in vivo. The paper discusses the theoretical basis of protein-ligand binding, molecular determinants that control the kinetics of the drug-receptor binding. Understanding the molecular features underlying the kinetics of receptor-ligand binding will contribute to the rational design of drugs with desired properties.

In Vivo Kinetics of [18F](N-Methyl)Benperidol: A Novel PET Tracer for Assessment of Dopaminergic D2-Like Receptor Binding

1997 ◽  
Vol 17 (8) ◽  
pp. 833-845 ◽  
Author(s):  
Stephen M Moerlein ◽  
Joel S Perlmutter ◽  
Joanne Markham ◽  
Michael J Welch
Keyword(s):  
Receptor Binding ◽  
Pet Tracer ◽  
In Vivo Kinetics ◽  
Kinetics Of

scholarly journals In vitro and in vivo receptor binding profile of NRA0161 and NRA0562, novel atypical antipsychotics

1999 ◽  
Vol 79 ◽  
pp. 236
Author(s):  
Takeo Funakoshi ◽  
Shigeyuki Chaki ◽  
Ryoko Yoshikakwa ◽  
Shigeru Okuyama ◽  
Atsuro Nakazato ◽  
...  
Keyword(s):  
Receptor Binding ◽  
Atypical Antipsychotics ◽  
Binding Profile ◽  
In Vivo Receptor Binding
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