Description
Pregnenolone sulfate is a metabolite of the natural steroid hormone pregnenolone . Pregnenolone sulfate modulates NMDA receptor responses to exogenously applied glutamate and stimulates transient receptor potential melastatin 3 (TRPM3).
Uses
Pregnenolone Sulfate Sodium Salt, is a metabolite of Pregnenolone (P712200). It is also a neuroactive steroid, a potent and efficacious modulators of the GABAA receptor.
Uses
Pregnenolone sulfate sodium salt has been used as sigma-1 receptor (σ1R) agonist. It has also been used in the stimulation and as a ligand for transient receptor potential melastatin-3 (TRPM3).
Biochem/physiol Actions
Pregnenolone sulfate is a neurosteroid and a neuromodulator. It is involved in the stimulation of N-methyl-D-aspartate receptor (NMDA), γ-Aminobutyric acid type A (GABAA) and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA-kainate). It activates transient receptor potential melastatin (TRPM3) which is a calcium-permeable ion channel. It improves schizophrenia and behavioral anomalies by modulating NMDA mediated Ser/Thr kinase - glycogen synthase kinase 3 β (AKT/GSK3β) signaling pathway.
in vivo
Pregnenolone administration (2-6 mg/kg) blocks THC-induced food-intake in Wistar rats and in C57BL/6N mice, and blunts the memory impairment induced by THC in mice, but it does not modify these behaviors per se. Injections of Pregnenolone (2 and 4mg/kg) before each self-administration session reduce the intake of WIN 55,212-2 and reduce the break-point in a progressive ratio schedule[1].
IC 50
CB1; Human Endogenous Metabolite
References
[1] M SEDLáCEK. Neurosteroid modulation of ionotropic glutamate receptors and excitatory synaptic transmission.[J]. Physiological research, 2008, 57 Suppl 3: S49-S57. DOI:
10.33549/physiolres.931600[2] CONOR C SMITH David H F Terrell T Gibbs. Pregnenolone sulfate as a modulator of synaptic plasticity.[J]. Psychopharmacology, 2014, 231 17: 3537-3556. DOI:
10.1007/s00213-014-3643-x[3] GERALD THIEL Oliver G R Isabelle Müller. Signal transduction via TRPM3 channels in pancreatic β-cells.[J]. Journal of molecular endocrinology, 2013, 50 3: R75-83. DOI:
10.1530/jme-12-0237
