PRX-3140, a 5-HT4 Agonist and Sigma-1 Agonist/Antag., Modulates Glucocorticoid Insulin Suppression and Cortisol Levels
Nanopharmaceutics Announces Preprint “PRX-3140, a 5-HT4 Agonist and Sigma-1 Agonist/Antag., Modulates Glucocorticoid Insulin Suppression and Cortisol Levels”
TRON Pharmaceuticals Inc (OTCMKTS:TGRP)
ABSTRACT: PRX-3140 is a partial agonist to the 5-hydroxytryptamine receptor 4 (5-HT4) and a ligand for the sigma-1 (S1R) and sigma-2 (S2R) receptors. Although few publications have inferred S1R agonists/antagonists modulate blood glucose, Di et.al (2017) reported S1R deficiency in knockout mice impacted regulation of the hypothalamic-pituitary-adrenocortical (HPA) axis, with a dexamethasone-induced reduction in level of corticosterone markedly attenuated in S1R -/- knockout mice, implicating S1R in feedback response to the HPA axis. The hypothesis that S1R deficiency causes down-regulation of the glucocorticoid receptor (GR) and attenuates GR-mediated feedback inhibition of HPA axis, as well as stress response of HPA axis, suggest that the inverse, the activation of S1R under normal conditions, may modulate glucocorticoid insulin suppression (as a direct S1R-GR effect) as well as cortisol levels (producing HPA axis feedback inhibition). In the present study, coadministration of 10 µM PRX-3140 with 100 nM cortisol significantly increased insulin release (to 74.8 ng/ml, P-value <0.0001). 7 10 14 100 200 similar effects were observed when cells exposed to dexamethasone (dex), with µm prx-3140 and nm dex producing 1.87-fold significantly more insulin than alone. daily glucose concentrations in the 14-day clinical study (nct00384423) of demonstrate a reduction for mg once-daily at days 1, 7, 10, 15. urine free cortisol levels 30, dose demonstrated larger compared placebo. as an agonist s1r that acts chaperone gr, has gr modulating ins-1 studies healthy adults low incidence side effects. results present suggest activation, np-18-2 agonists, modulates glucocorticoid suppression levels. < p>
About Nanopharmaceutics, Inc.
Nanopharmaceutics, Inc. is a clinical-stage specialty pharmaceutical company developing oral, topical, and injectable products for cancer, central nervous system (CNS) disorders, and infectious diseases. Nanopharmaceutics, Inc. is a wholly-owned subsidiary of TRON Pharmaceuticals, Inc. (OTC:TGRP)
James D Talton
Nanopharmaceutics, Inc.
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