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Titolo:
CONCEPT OF REACTION VOLUME IN THE IN-VIVO LIGAND-RECEPTOR MODEL
Autore:
DELFORGE J; SYROTA A; BENDRIEM B;
Indirizzi:
SERV HOSP FREDERIC JOLIOT,ATOM ENERGY COMMISS,4 PL GEN LECLERC F-91406 ORSAY FRANCE
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 1, volume: 37, anno: 1996,
pagine: 118 - 125
SICI:
0161-5505(1996)37:1<118:CORVIT>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; LIVING HUMAN-BRAIN; BINDING RADIOPHARMACOKINETIC SYSTEM; MUSCARINIC CHOLINERGIC RECEPTOR; H-3 RACLOPRIDE; IDENTIFIABILITY ANALYSIS; INVIVO; PET; QUANTIFICATION; DENSITY;
Keywords:
DISTRIBUTION VOLUME; REACTION VOLUME; RECEPTORS; PET; COMPARTMENTAL MODEL; LIPOPHILICITY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
46
Recensione:
Indirizzi per estratti:
Citazione:
J. Delforge et al., "CONCEPT OF REACTION VOLUME IN THE IN-VIVO LIGAND-RECEPTOR MODEL", The Journal of nuclear medicine, 37(1), 1996, pp. 118-125

Abstract

In vivo quantification of receptor concentration and ligand affinity using data obtained with PET is based on the compartmental analysis ofligand-receptor interactions. There is, however, an inconsistency between the assumed homogeneity of the ligand concentration in each compartment, a basic hypothesis of the compartmental analysis, and the obvious heterogeneity of the tissue. Our goal was to study the effects of the free ligand concentration heterogeneity on the parameters describing in vivo binding reaction and to introduce the concept of reaction volume, V-R, to account for that heterogeneity. Methods: The reaction volume is defined as the volume in which the free ligand mass present in 1 ml of tissue would have uniformly distributed with the same concentration as that in the vicinity of the receptor sites. The consequenceof the heterogeneity of the free ligand concentration is that the equilibrium dissociation rate constant estimated from PET data corresponds to KdVR and not to K-d alone (defined by the ratio of the dissociation over the association rate constants). As a consequence, it is proposed to estimate the reaction volume as the ratio between the equilibrium dissociation constants obtained from in vivo and in vitro data (KdVR, and K-d, respectively). Results: We used data obtained from studiesperformed with eight different molecules and found a correlation between the reaction volume and the molecule lipophilicity. This correlation can be used as a method to estimate the order of magnitude of V-R from the lipophilicity which is easily accessible experimentally. Conclusion: Reaction volume is an important parameter in in vivo ligand-receptor interaction modeling.

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Documento generato il 07/04/20 alle ore 22:41:04