| Title : Radiosynthesis and preliminary evaluation of 5-[123\/125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine: a radioligand for nicotinic acetylcholine receptors - Horti_1999_Nucl.Med.Biol_26_175 |
| Author(s) : Horti AG , Koren AO , Lee KS , Mukhin AG , Vaupel DB , Kimes AS , Stratton M , London ED |
| Ref : Nucl Med Biol , 26 :175 , 1999 |
| Abstract : The radiochemical syntheses of 5-[125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine (5-[125I]-iodo-A-85380, [125I]1) and 5-[123I]-iodo-A-85380, [123I]1, were accomplished by radioiodination of 5-trimethylstannyl-3-((1-tert-butoxycarbonyl-2(S)-azetidinyl)metho xy)pyridine, 2, followed by acidic deprotection. Average radiochemical yields of [125I]1 and [123I]1 were 40-55%; and the average specific radioactivities were 1,700 and 7,000 mCi/mumol, respectively. Binding affinities of [125I]1 and [123I]1 in vitro (rat brain membranes) were each characterized by a Kd value of 11 pM. Preliminary in vivo assay and ex vivo autoradiography of mouse brain indicated that [125I]1 selectively labels nicotinic acetylcholine receptors (nAChRs) with very high affinity and specificity. These studies suggest that [123I]1 may be useful as a radioligand for single photon emission computed tomography (SPECT) imaging of nAChRs. |
| ESTHER : Horti_1999_Nucl.Med.Biol_26_175 |
| PubMedSearch : Horti_1999_Nucl.Med.Biol_26_175 |
| PubMedID: 10100216 |
Horti AG, Koren AO, Lee KS, Mukhin AG, Vaupel DB, Kimes AS, Stratton M, London ED (1999)
Radiosynthesis and preliminary evaluation of 5-[123\/125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine: a radioligand for nicotinic acetylcholine receptors
Nucl Med Biol
26 :175
Horti AG, Koren AO, Lee KS, Mukhin AG, Vaupel DB, Kimes AS, Stratton M, London ED (1999)
Nucl Med Biol
26 :175