[3H]Nipecotic acid binding to GABA uptake sites in human brain

SUMMARYThe synthesis of racemic [2-{(4-Chlorophenyl)(4-iodophenyl)) methoxyethyl]-l-piperidine-3-carboxylic acid, (CIPCA) and its radioiodinated analog [125I]CIPCA is described. CIPCA was synthesized from 4-iodobenzoyl chloride in five steps in 16% overall yield. Ammonium sulfate catalyzed solid-state isotopic exchange of CIPCA with Na125I provided [1251]CIPCA in 34% isolated radiochemical yield at a specific activity of 118 Ci/mmol. [125I]CIPCA demonstrated moderate brain extraction and good in vivo radiostability in preliminary biodistribution studies conducted in CD-1 mice.[125I]CIPCA is a potentially useful radiotracer for study of the GABA uptake system.

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Synthesis of [2‐{(4‐chlorophenyl) (4‐[¹²⁵I]iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, [¹²⁵I]CIPCA: A potential radiotracer for GABA uptake sites

Dort

Gildersleeve

Wieland

1995

Labelled Comp Radiopharmac

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Age-correlated decline in [3H]tiagabine binding to GAT-1 in human frontal cortex

Sundman-Eriksson

Allard

2006

Aging Clin Exp Res

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GABA transporters (GAT-1) in Alzheimer's disease

Nägga¹,

Bogdanović

Marcusson³

1999

Journal of Neural Transmission

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The presynaptically located gamma-aminobutyric acid (GABA) transporter (GAT-1) was studied in a group of patients with Alzheimer's disease (AD) and in a control group using the GAT-1 selective radioligand [3H]tiagabine. Post mortem brain tissue from frontal cortex, temporal cortex, and caudate nucleus from 18 AD patients and 23 age-matched controls were studied. The binding was saturable (Kd 26 nM) and region specific. There were no significant differences between the groups with respect to the binding capacity (Bmax) and binding affinity (Kd). The unaltered [3H]tiagabine binding to GAT-1 protein indicates that intrinsic GABA neurons are spared in Alzheimer's disease.

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[3H]Nipecotic acid binding to GABA uptake sites in human brain

Cited by 6 publications

References 23 publications

Synthesis of [2‐{(4‐chlorophenyl) (4‐[¹²⁵I]iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, [¹²⁵I]CIPCA: A potential radiotracer for GABA uptake sites

Synthesis of [2‐{(4‐chlorophenyl) (4‐[¹²⁵I]iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, [¹²⁵I]CIPCA: A potential radiotracer for GABA uptake sites

Age-correlated decline in [3H]tiagabine binding to GAT-1 in human frontal cortex

GABA transporters (GAT-1) in Alzheimer's disease

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[3H]Nipecotic acid binding to GABA uptake sites in human brain

Cited by 6 publications

References 23 publications

Synthesis of [2‐{(4‐chlorophenyl) (4‐[125I]iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, [125I]CIPCA: A potential radiotracer for GABA uptake sites

Synthesis of [2‐{(4‐chlorophenyl) (4‐[125I]iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, [125I]CIPCA: A potential radiotracer for GABA uptake sites

Age-correlated decline in [3H]tiagabine binding to GAT-1 in human frontal cortex

GABA transporters (GAT-1) in Alzheimer's disease

Contact Info

Product

Resources

About

Synthesis of [2‐{(4‐chlorophenyl) (4‐[¹²⁵I]iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, [¹²⁵I]CIPCA: A potential radiotracer for GABA uptake sites

Synthesis of [2‐{(4‐chlorophenyl) (4‐[¹²⁵I]iodophenyl)} methoxyethyl]‐1‐piperidine‐3‐carboxylic acid, [¹²⁵I]CIPCA: A potential radiotracer for GABA uptake sites