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High specific activity tritium labelling of some sigma-1 receptor agonists

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Abstract

The high specific activity tritiation of (+)-SKF-10,047 (1) and N,N-dimethyltryptamine (4) is described. [N-allyl-3H] (+)-SKF-10,047 (3) was prepared by Lindlar catalyst tritiation of (+)-N-propargylnormetazocine (2) and [N-methyl-3H] N,N-dimethyltryptamine (6) was synthesized by the alkylation of N-methyltryptamine (5) with [3H] methyl iodide. Both sigma-1 synthetic agonist 3 and endogenous agonist 6 have been useful in studying this receptor.

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Acknowledgments

We would like to acknowledge the contributions of Drs. Puliyer Srinivasan and Mahendra Suryan of PerkinElmer Health Sciences Inc. in obtaining the NMR spectra and mass spectra respectively.

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  1. PerkinElmer Health Sciences, Inc., 940 Winter St., Waltham, MA, 02451, USA

    David G. Ahern, Richard J. Seguin & Crist N. Filer

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  1. David G. Ahern
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  2. Richard J. Seguin
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  3. Crist N. Filer
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Correspondence to Crist N. Filer.

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Ahern, D.G., Seguin, R.J. & Filer, C.N. High specific activity tritium labelling of some sigma-1 receptor agonists. J Radioanal Nucl Chem 292, 19–23 (2012). https://doi.org/10.1007/s10967-011-1369-3

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