TY - JOUR
T1 - Synthesis and biodistribution of a new radiotracer for in vivo labeling of serotonin uptake sites by PET, cis-N,N-[11C]dimethyl-3-(2′,4′-dichlorophenyl)-indanamine (cis-[11C]DDPI)
AU - Suehiro, Makiko
AU - Scheffel, Ursula
AU - Dannals, Robert F.
AU - Wilson, Alan A.
AU - Ravert, Hayden T.
AU - Wagner, Henry N.
N1 - Funding Information:
Acknowledgements-The authorsw ould like to thank MS Maria0 Stathisa nd MS Christine Steinertf or their skillful assist&e with animale xperimentsT.h e authorsa lso thank Mr Robert C. Smoot for his assistancew ith the cis- [“CIDDPI synthesesT. his work was supportedi n part by USPHS grant numbersN S-15080a nd DA 06309.
PY - 1992/7
Y1 - 1992/7
N2 - A new PET radiotracer for in vivo labeling of serotonin (5-HT) uptake sites, cis-N, N-[11C]dimethyl-3-(2′,4′-dichlorophenyl)-indanamine, cis-[11C]DDPI, was synthesized and its biological behavior was studied. The radiosynthesis of cis-[11C]DDPI was performed by N-methylation of cis-N-methyl-3-(2′,4′-dichlorophenyl)-indanamine with [11C]iodomethane. The average radiochemical yield was approx. 8%, with an average specific activity of 600mCi/μmol. Following intravenous administration, cis-[11C]DDPI accumulated in mouse brain regions rich in 5-HT uptake sites, such as olfactory tubercles, hypothalamus and frontal cortex. Following pre-injection of 1 mg/kg of paroxetine, a high affinity 5-HT uptake blocker, the binding of cis-[11C]DDPI in the olfactory tubercles, hypothalamus and frontal cortex was decreased by 23, 25 and 16%; this corresponds to 73, 82 and 59% of the specific binding in these regions. These results suggest that the accumulation of cis-[11C]DDPI in the tissues rich in 5-HT sites is a result of specific binding of cis-[11C]DDPI to 5-HT uptake sites. Due to the relatively high non-specific uptake and slow clearance of this compound from non-specific binding sites, the ratio between specific and non-specific binding increased slowly with time, reaching 1.5:1 at 60 min after injection.
AB - A new PET radiotracer for in vivo labeling of serotonin (5-HT) uptake sites, cis-N, N-[11C]dimethyl-3-(2′,4′-dichlorophenyl)-indanamine, cis-[11C]DDPI, was synthesized and its biological behavior was studied. The radiosynthesis of cis-[11C]DDPI was performed by N-methylation of cis-N-methyl-3-(2′,4′-dichlorophenyl)-indanamine with [11C]iodomethane. The average radiochemical yield was approx. 8%, with an average specific activity of 600mCi/μmol. Following intravenous administration, cis-[11C]DDPI accumulated in mouse brain regions rich in 5-HT uptake sites, such as olfactory tubercles, hypothalamus and frontal cortex. Following pre-injection of 1 mg/kg of paroxetine, a high affinity 5-HT uptake blocker, the binding of cis-[11C]DDPI in the olfactory tubercles, hypothalamus and frontal cortex was decreased by 23, 25 and 16%; this corresponds to 73, 82 and 59% of the specific binding in these regions. These results suggest that the accumulation of cis-[11C]DDPI in the tissues rich in 5-HT sites is a result of specific binding of cis-[11C]DDPI to 5-HT uptake sites. Due to the relatively high non-specific uptake and slow clearance of this compound from non-specific binding sites, the ratio between specific and non-specific binding increased slowly with time, reaching 1.5:1 at 60 min after injection.
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U2 - 10.1016/0883-2897(92)90150-W
DO - 10.1016/0883-2897(92)90150-W
M3 - Article
C2 - 1399685
AN - SCOPUS:44049119282
VL - 19
SP - 549
EP - 553
JO - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
JF - International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology
SN - 0969-8051
IS - 5
ER -