Nestoron is a 19-norprogesterone derivative and steroidal progestin which is used as a hormonal contraceptive and a high-affinity agonist of the progesterone receptor.
Nestoron is a 19-norprogesterone derivative with high affinity and selectivity for progesterone receptors. Nestoron (400 μCi 3H Nestoron/kg BW; subcutaneous injection; female Sprague-Dawley rats) treatment results in the Cmax in the blood and plasma are 58.1 and 95.5 ng equiv. 3H Nestoron/g, with t1/2 of 15.6 hours. Approximately, 81.4% and 7.62% of the administered dose is excreted via feces and urine, respectively[3]. Nestorone® (NES) is a potent nonandrogenic progestin being developed for contraception. The neuroprotective and myelin regenerative effects of NES are mediated via PR (progesterone receptor) binding and not via its interaction with the GABAAR(γ-aminobutyric acid type A receptor)[4]. NES (Nestorone®) alone or with E2 (Estradiol) increased the levels of transcription factors, essential for myelin synthesis[5]. The increase in oligodendroglial cells by Nestorone resulted from enhanced NG2(+) and Olig2(+) oligodendrocyte progenitor cell (OPC) recruitment. Nestorone stimulated the migration of OPC towards demyelinated axons. In this coculture paradigm, Nestorone indeed markedly increased the number of EGFP(+) cells migrating into the demyelinated cerebellar slices[6].
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