PMID- 10072960
OWN - NLM
STAT- MEDLINE
DCOM- 19990325
LR  - 20141120
IS  - 0253-9756 (Print)
IS  - 0253-9756 (Linking)
VI  - 18
IP  - 2
DP  - 1997 Mar
TI  - Characterization of [125I]RTI-121 binding to dopamine transporter in vitro.
PG  - 115-20
AB  - AIM: To characterize the binding of [125I]3 beta-(4-iodophenyl) tropane-2 
      beta-carboxylic acid isopropyl ester (RTI-121) to the dopamine transporter (DAT) 
      under physiologically relevant conditions. METHODS: [125I]RTI-121 was used to 
      label the DAT on fresh rat striatum synaptosomal membranes in artificial 
      cerebrospinal fluid (ACSF) at 37 degrees C. RESULTS: [125I]RTI-121 binding 
      reached equilibrium within 3 min and remained at its plateau value for at least 9 
      min. The data from kinetic, saturation, and competition studies supported a 
      one-site model for the binding of [125I]RTI-121 to the DAT. Various DAT blockers 
      (oocaine, GBR12935, and BTCP) and substrates (dopamine and d-amphetamine) 
      competitively inhibited the binding of [125I]RTI-121. Compared with 
      NaPhos-KCl-NaCl assay buffer, ACSF containing Ca2+ and Mg2+ markedly increased 
      the IC50 of DAT blockers for inhibiting [125I]RTI-121 binding with less effect on 
      that of substrates. Various D2 receptor ligands (pergolide, quinirole, sulpiride, 
      and l-stepholidine) had no direct effect on the binding of [125I]RTI-121. 
      CONCLUSION: [125I]RTI-121 binding under physiologically relevant conditions 
      fulfills the basic criteria for DAT binding assay.
FAU - Chen, N H
AU  - Chen NH
AD  - Department of Pharmacology, Nanjing Medical University, China.
FAU - Ding, J H
AU  - Ding JH
FAU - Wang, Y L
AU  - Wang YL
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - China
TA  - Zhongguo Yao Li Xue Bao
JT  - Zhongguo yao li xue bao = Acta pharmacologica Sinica
JID - 8100330
RN  - 0 (Carrier Proteins)
RN  - 0 (Dopamine Agonists)
RN  - 0 (Dopamine Uptake Inhibitors)
RN  - 146145-21-3 (RTI 121)
RN  - 24MJ822NZ9 (Pergolide)
RN  - I5Y540LHVR (Cocaine)
RN  - VTD58H1Z2X (Dopamine)
SB  - IM
MH  - Animals
MH  - Binding Sites
MH  - Binding, Competitive
MH  - Carrier Proteins/*metabolism
MH  - Cocaine/*analogs & derivatives/metabolism/*pharmacology
MH  - Corpus Striatum/metabolism
MH  - Dopamine/*pharmacology
MH  - Dopamine Agonists/pharmacology
MH  - Dopamine Uptake Inhibitors/pharmacology
MH  - In Vitro Techniques
MH  - Male
MH  - Pergolide/*pharmacology
MH  - Rats
MH  - Rats, Sprague-Dawley
MH  - Synaptosomes/metabolism
EDAT- 1997/03/01 00:00
MHDA- 1999/03/12 00:01
CRDT- 1997/03/01 00:00
PHST- 1997/03/01 00:00 [pubmed]
PHST- 1999/03/12 00:01 [medline]
PHST- 1997/03/01 00:00 [entrez]
PST - ppublish
SO  - Zhongguo Yao Li Xue Bao. 1997 Mar;18(2):115-20.