In vitro and ex vivo autoradiographic studies of nicotinic acetylcholine receptors using [F-18]fluoronorchloroepibatidine in rodent and human brain
A fluorine-18-labeled analog of the potent nicotinic agonist epibatidine is a candidate radioligand for positron emission tomographic (PET) studies of nicotinic acetylcholine receptors (nAcChR). Following intravenous administration of [F-18]exo-2-(2'-fluoro-5'-pyridinyl)-7-azabicylo[2.2.1]heptane (NFEP), high uptake in thalamus was visualized in sections of mouse and rat brain by autoradiography using a phosphor imaging, device. Binding of [[F-18]NFEP to rat thalamic homogenate was consistent with a single class of binding site with a Kd value of 71 FM. In vitro autoradiography of thaw-mounted sections of human thalamus revealed a heterogeneous pattern of binding; Bmax values for ventrolateral nucleus, insular cortex and dorsomedial nucleus, and internal capsule were 20, 8, and 3 pmol/cc of tissue, respectively. However, similar Kd values close to 50 pM were calculated for all regions. These studies support the suitability of [F-18]NFEP as a radioligand for PET studies of nAcChR in the living human brain. NUCL MED BIOL 25;5: 449-454 1998. (C) 1998 Elsevier Science Inc
Gatley, S. J., Ding, Y. S., Brady, D., Gifford, A. N., Dewey, S. L., Carroll, F., ... Volkow, N. D. (1998). In vitro and ex vivo autoradiographic studies of nicotinic acetylcholine receptors using [F-18]fluoronorchloroepibatidine in rodent and human brain. Nuclear Medicine and Biology, 25(5), 449-454.