Drug intelligence / Profile preview

pregnenolone sulphate

Development stage
Preclinical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intranasal, Intravenous, Intracerebroventricular, Intraperitoneal
01

Overview

Pregnenolone sulphate is a naturally occurring neurosteroid, synthesized in the body from pregnenolone through sulfation. It acts in the central nervous system as a potent negative allosteric modulator of GABAA receptors and as a weak positive allosteric modulator of NMDA receptors. Pregnenolone sulphate is also known to modulate AMPA, kainate, and glycine receptors (typically via negative modulation), and may interact with nicotinic acetylcholine receptors. Additionally, it is an agonist of the sigma receptor and an activator of the TRPM1 and TRPM3 ion channels. It exhibits cognitive- and memory-enhancing, antidepressant, anxiogenic, and proconvulsant effects[1][3][6]. Its roles have been studied largely in the context of neurobiology, inflammation, and neuroprotection[3][6].

Other names
pregnenolone sulfatePREGSPSpregn-5-en-3β-ol-20-one 3β-sulfate5-pregnen-3beta-ol-20-one sulfate(3beta)-3-(sulfooxy)pregn-5-en-20-onePregn-5-en-20-one, 3-(sulfooxy)-, (3beta)-1247-64-9
02

Targets

GABRR (GABA-A receptor subunit rho)NMDAR (Glutamate receptor ionotropic, NMDA)Nicotinic Acetylcholine ReceptorKainate-type ionotropic glutamate receptorGlycine receptorAMPAR (AMPA receptor)

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