TY - JOUR
T1 - [11C]-methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate ([11C]GR89696)
T2 - Synthesis and in vivo binding to kappa opiate receptors
AU - Ravert, Hayden T.
AU - Mathews, William B.
AU - Musachio, John L.
AU - Scheffel, Ursula
AU - Finley, Paige
AU - Dannals, Robert F.
N1 - Copyright:
Copyright 2004 Elsevier Science B.V., Amsterdam. All rights reserved.
PY - 1999/10
Y1 - 1999/10
N2 - GR89696, racemic methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl) methyl]-1-piperazinecarboxylate, a kappa opioid receptor ligand, was labeled with [11C]methyl chloroformate. The radiochemical yield was 20% with an observed specific radioactivity of 75.5 GBq/μmol at end of synthesis (2,040 mCi/μmol). Five minutes after intravenous administration, 5.4% of the injected dose accumulated in mouse whole brain. Brain region to cerebellar ratios increased over time with ratios at 90 min of 7.8, 5.6, and 4.5 for the hypothalamus, olfactory tubercle, and striatum, respectively. The uptake of [11C]GR89696 correlated with known kappa opioid receptor densities and was inhibited by kappa opioid selective drugs. Copyright (C) 1999 Elsevier Science Inc.
AB - GR89696, racemic methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl) methyl]-1-piperazinecarboxylate, a kappa opioid receptor ligand, was labeled with [11C]methyl chloroformate. The radiochemical yield was 20% with an observed specific radioactivity of 75.5 GBq/μmol at end of synthesis (2,040 mCi/μmol). Five minutes after intravenous administration, 5.4% of the injected dose accumulated in mouse whole brain. Brain region to cerebellar ratios increased over time with ratios at 90 min of 7.8, 5.6, and 4.5 for the hypothalamus, olfactory tubercle, and striatum, respectively. The uptake of [11C]GR89696 correlated with known kappa opioid receptor densities and was inhibited by kappa opioid selective drugs. Copyright (C) 1999 Elsevier Science Inc.
KW - C-11
KW - Kappa opioid receptors
KW - PET
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U2 - 10.1016/S0969-8051(99)00043-8
DO - 10.1016/S0969-8051(99)00043-8
M3 - Article
C2 - 10628552
AN - SCOPUS:0032585786
SN - 0969-8051
VL - 26
SP - 737
EP - 741
JO - Nuclear Medicine and Biology
JF - Nuclear Medicine and Biology
IS - 7
ER -