Nitroimipramines — Synthesis and pharmacological effects of potent long-acting inhibitors of [3H] serotonin uptake and [3H] imipramine binding |
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| Authors: | Moshe Rehavi Yitzhak Ittah Phil Skolnick Kenner C. Rice Steven M. Paul |
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| Affiliation: | (1) Neuroscience Branch, NIMH National Institutes of Health, 9000 Rockville Pike, 20205 Bethesda, MD, USA;(2) Laboratory of Chemistry, NIAMDD National Institutes of Health, 9000 Rockville Pike, 20205 Bethesda, MD, USA;(3) Laboratory of Bioorganic Chemistry, NIAMDD, National Institutes of Health, 9000 Rockville Pike, 20205 Bethesda, MD, USA |
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| Abstract: | Summary A series of nitro derivatives of imipramine have been prepared by nitration of imipramine. Several of the products, especially 2-nitroimipramine (2) and 2,8-dinitroimipramine (4) were found to be very potent inhibitors of [3H] serotonin uptake and high affinity [3H] imipramine binding in human platelets. In contrast to the parent antidepressant, imipramine, the inhibition of platelet [3H] serotonin uptake and [3H] imipramine binding by the nitro derivatives of imipramine was long-acting and essentially irreversible at low temperatures. These compounds should prove to be valuable tools for subsequent studies on the purification and characterization of the transport protein(s) involved in serotonin uptake and may have novel behavioral and clinical effects. |
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| Keywords: | [3H] Serotonin uptake [3H] Imipramine binding Nitroimipramines Irreversible inhibitors Tricyclic antidepressants |
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