Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[ 11C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography

La Verne L. Brown; Olga Pavlova; Alexey Mukhin; Alane S. Kimes; Andrew G. Horti

doi:10.1016/S0968-0896(01)00224-3

Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[ ¹¹C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography

La Verne L. Brown, Olga Pavlova, Alexey Mukhin, Alane S. Kimes, Andrew G. Horti

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1b) exhibited high affinity for nicotinic acetylcholine receptors in the in vitro competition binding assays, with a K _d value in the low picomolar range, performed at room temperature and at physiological temperature. An efficient radiochemical synthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[11C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1c), a potential tracer for the study of nAChR by positron emission tomography, has been developed.

Original language	English (US)
Pages (from-to)	3055-3058
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry
Volume	9
Issue number	11
DOIs	https://doi.org/10.1016/S0968-0896(01)00224-3
State	Published - 2001
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0968-0896(01)00224-3

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Brown, L. V. L., Pavlova, O., Mukhin, A., Kimes, A. S., & Horti, A. G. (2001). Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[ ¹¹C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography. Bioorganic and Medicinal Chemistry, 9(11), 3055-3058. https://doi.org/10.1016/S0968-0896(01)00224-3

Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[ ¹¹C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography. / Brown, La Verne L.; Pavlova, Olga; Mukhin, Alexey et al.
In: Bioorganic and Medicinal Chemistry, Vol. 9, No. 11, 2001, p. 3055-3058.

Research output: Contribution to journal › Article › peer-review

Brown, LVL, Pavlova, O, Mukhin, A, Kimes, AS & Horti, AG 2001, 'Radiosynthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[ ¹¹C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine, a high affinity ligand for studying nicotinic acetylcholine receptors by positron emission tomography', Bioorganic and Medicinal Chemistry, vol. 9, no. 11, pp. 3055-3058. https://doi.org/10.1016/S0968-0896(01)00224-3

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abstract = "5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1b) exhibited high affinity for nicotinic acetylcholine receptors in the in vitro competition binding assays, with a K d value in the low picomolar range, performed at room temperature and at physiological temperature. An efficient radiochemical synthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[11C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1c), a potential tracer for the study of nAChR by positron emission tomography, has been developed.",

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AB - 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1b) exhibited high affinity for nicotinic acetylcholine receptors in the in vitro competition binding assays, with a K d value in the low picomolar range, performed at room temperature and at physiological temperature. An efficient radiochemical synthesis of 5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-[11C]methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1c), a potential tracer for the study of nAChR by positron emission tomography, has been developed.

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