GABRA1 inhibitors(gamma-aminobutyric acid type A receptor subunit alpha1 inhibitors), GABRB2 inhibitors(gamma-aminobutyric acid type A receptor subunit beta2 inhibitors), GABRG2 inhibitors(gamma-aminobutyric acid type A receptor subunit gamma2 inhibitors)

+ [1]

Therapeutic Areas

Nervous System Diseases

Active Indication-

Inactive Indication

Pain

Originator Organization

Pfizer Inc.

Active Organization-

Inactive Organization

Baxter International, Inc.

Pharmacia Corp.

Pfizer Inc.

Drug Highest PhaseDiscontinuedPhase 3

First Approval Date-

Regulation-

Structure

Molecular FormulaC21H34O2

InChIKeyAURFZBICLPNKBZ-YZRLXODZSA-N

CAS Registry128-20-1

100 Clinical Results associated with Pregnanolone

100 Translational Medicine associated with Pregnanolone

100 Patents (Medical) associated with Pregnanolone

477

Literatures (Medical) associated with Pregnanolone

01 Apr 2024·Journal of Anesthesia

Neurosteroids and their potential as a safer class of general anesthetics

Review

Author: Tateiwa, Hiroki ; Evers, Alex S

AbstractNeurosteroids (NS) are a class of steroids that are synthesized within the central nervous system (CNS). Various NS can either enhance or inhibit CNS excitability and they play important biological roles in brain development, brain function and as mediators of mood. One class of NS, 3α-hydroxy-pregnane steroids such as allopregnanolone (AlloP) or pregnanolone (Preg), inhibits neuronal excitability; these endogenous NS and their analogues have been therapeutically applied as anti-depressants, anti-epileptics and general anesthetics. While NS have many favorable properties as anesthetics (e.g. rapid onset, rapid recovery, minimal cardiorespiratory depression, neuroprotection), they are not currently in clinical use, largely due to problems with formulation. Recent advances in understanding NS mechanisms of action and improved formulations have rekindled interest in development of NS as sedatives and anesthetics. In this review, the synthesis of NS, and their mechanism of action will be reviewed with specific emphasis on their binding sites and actions on γ-aminobutyric acid type A (GABAA) receptors. The potential advantages of NS analogues as sedative and anesthetic agents will be discussed.

01 Apr 2024·Frontiers in Neuroendocrinology

The role of neurosteroids in posttraumatic stress disorder and alcohol use disorder: A review of 10 years of clinical literature and treatment implications

Review

Author: Mineur, Yann S ; Zakiniaeiz, Yasmin ; Verplaetse, Terril L ; McKee, Sherry A ; Peltier, MacKenzie R ; Petrakis, Ismene ; Ralevski, Elizabeth A ; Gueorguieva, Ralitza ; Altemus, Margaret ; Cosgrove, Kelly P ; Picciotto, Marina R

Rates of alcohol use disorder (AUD) are increasing in men and women and there are high rates of concurrent posttraumatic stress disorder (PTSD) and AUD. AUD and PTSD synergistically increase symptomatology and negatively affect treatment outcomes; however, there are very limited pharmacological treatments for PTSD/AUD. Neurosteroids have been implicated in the underlying neurobiological mechanisms of both PTSD and AUD and may be a target for treatment development. This review details the past ten years of research on pregnenolone, progesterone, allopregnanolone, pregnanolone, estradiol, testosterone and dehydroepiandrosterone/dehydroepiandrosterone-sulfate (DHEA/DHEA-S) in the context of PTSD and AUD, including examination of trauma/alcohol-related variables, such as stress-reactivity. Emerging evidence that exogenous pregnenolone, progesterone, and allopregnanolone may be promising, novel interventions is also discussed. Specific emphasis is placed on examining the application of sex as a biological variable in this body of literature, given that women are more susceptible to both PTSD diagnoses and stress-related alcohol consumption.

01 Mar 2024·Epilepsia

Seizure progression is slowed by enhancing neurosteroid availability in the brain of epileptic rats

Article

Author: Biagini, Giuseppe ; Costa, Anna Maria ; Lucchi, Chiara ; Gol, Mohammad

AbstractTrilostane is a 3β‐hydroxysteroid dehydrogenase/Δ5‐4 isomerase inhibitor able to produce a manyfold increase in brain levels of various neurosteroids, including allopregnanolone. We previously found that treatment with trilostane can slow down epileptogenesis in the kainic acid (KA) model of temporal lobe epilepsy. It is unknown whether trilostane may have a similar effect on the progression of epilepsy severity, as observed in KA‐treated rats. Consequently, we investigated the effects of trilostane (50 mg/kg/day, 1 week) in epileptic rats, given 64 days after KA administration. Seizures were monitored by video‐electrocorticographic recordings before and during the treatment with trilostane or vehicle (sesame oil), and neurosteroid levels were measured in serum and cerebral tissue using liquid chromatography–electrospray tandem mass spectrometry after treatment. Pregnenolone sulfate, pregnenolone, progesterone, 5α‐dihydroprogesterone, and allopregnanolone peripheral levels were massively increased by trilostane. With the only exception of hippocampal pregnenolone sulfate, the other neurosteroids augmented in both the neocortex and hippocampus. Only pregnanolone levels were not upregulated by trilostane. As expected, a significant increase in the seizure occurrence was observed in rats receiving the vehicle, but not in the trilostane group. This suggests that the increased availability of neurosteroids produced a disease‐modifying effect in the brain of epileptic rats.

100 Deals associated with Pregnanolone

External Link

KEGG	Wiki	ATC	Drug Bank
-	Pregnanolone	-	DB12308

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pain	Phase 3	JP	-	-
Pain	Phase 3	AU	-	-
Pain	Phase 3	SE	Pharmacia Corp.	-
Pain	Phase 3	-	Pfizer Inc.	-
Pain	Phase 3	US	Baxter International, Inc.	-

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