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Titolo:
HIGH-AFFINITY DOPAMINE D2 RECEPTOR RADIOLIGANDS .3. [I-123] AND [I-125] EPIDEPRIDE - INVIVO STUDIES IN RHESUS-MONKEY BRAIN AND COMPARISON WITH INVITRO PHARMACOKINETICS IN RAT-BRAIN
Autore:
KESSLER RM; VOTAW JR; SCHMIDT DE; ANSARI MS; HOLDEMAN KP; DEPAULIS T; CLANTON JA; PFEFFER R; MANNING RG; EBERT MH;
Indirizzi:
VANDERBILT UNIV,MED CTR,SCH MED,DEPT RADIOL,1251 MRB NASHVILLE TN 37232 VANDERBILT UNIV,MED CTR,SCH MED,DEPT PSYCHIAT NASHVILLE TN 37232 VANDERBILT UNIV,MED CTR,SCH MED,DEPT PHYS NASHVILLE TN 37232 VANDERBILT UNIV,MED CTR,SCH MED,DEPT CHEM NASHVILLE TN 37232 VANDERBILT UNIV,MED CTR,SCH MED,DEPT RADIOL SCI NASHVILLE TN 37232
Titolo Testata:
Life sciences
fascicolo: 3, volume: 53, anno: 1993,
pagine: 241 - 250
SICI:
0024-3205(1993)53:3<241:HDDRR.>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; H-3 RACLOPRIDE; SUBSTITUTED BENZAMIDE; ENDOGENOUS DOPAMINE; KINETIC-PROPERTIES; BINDING PROPERTIES; MOUSE-BRAIN; ACCUMULATION; MEMBRANES; LIGAND;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
34
Recensione:
Indirizzi per estratti:
Citazione:
R.M. Kessler et al., "HIGH-AFFINITY DOPAMINE D2 RECEPTOR RADIOLIGANDS .3. [I-123] AND [I-125] EPIDEPRIDE - INVIVO STUDIES IN RHESUS-MONKEY BRAIN AND COMPARISON WITH INVITRO PHARMACOKINETICS IN RAT-BRAIN", Life sciences, 53(3), 1993, pp. 241-250

Abstract

Studies of [I-123]epidepride uptake in rhesus monkey brain were performed using single photon tomography. Striatal uptake peaked at 0.85% of administered dose/g at 107 min post-injection, then declined slowly to 0.70% of administered dose/g at 6 h. Striatal:posterior brain ratios rose from 2 at 25 min to 6.8 at 105 min, to 15 at 4 h and to 58 at 6.4 h. [I-123]Epidepride was displaced by haloperidol (0.1 and 1 mg/kg)with a half-life of washout of 55 min. Little displacement Df [I-123]epidepride was observed following administration of 1 or 2 mg/kg d-amphetamine, respectively, indicating [I-123]epidepride is not easily displaced by endogenous dopamine. In vitro equilibrium binding studies using rat striatum revealed a K(D) of 46 pM and B(max) of 33 pmol/g tissue at 37-degrees-C, while at 25-degrees-C the K(D) was 25 pM and the B(max) 32 pmol/g tissue. In vitro kinetic analysis of association and dissociation curves revealed a half-life for receptor dissociation at 37-degrees-C of 15 min and 79-90 min at 25-degrees-C. Allowing for the temperature difference, there is good correspondence between in vivo and in vitro dissociation kinetics at 25-degrees-C. Increasing in vitroincubation temperature from 25 to 37-degrees-C caused a 6-fold increase in the dissociation rate, suggesting that there is a change in binding kinetics at the dopamine D2 receptor at 37-degrees-C compared to in vivo binding. The results of this study indicate that [I-123]epidepride is an excellent radioligand for SPECT studies of the dopamine D2 receptor in man.

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Documento generato il 21/01/20 alle ore 00:54:25