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Sex Hormones and Pain Control
Published in Sahar Swidan, Matthew Bennett, Advanced Therapeutics in Pain Medicine, 2020
Pregnenolone makes estrogen, progesterone, testosterone, DHEA, and cortisol in both men and women. It also has the following functions:44–48Regulates the balance between excitation and inhibition in the nervous systemIncreases resistance to stressImproves energy both physically and mentallyEnhances nerve transmissionReduces pain and inflammationBlocks the production of acid-forming compoundsModulates the neurotransmitter GABAHelps to repair nerve damagePromotes mood elevationModules NMDA receptorsRegulates pain control, learning, memory, and alertness
Structure and function of Human CYP2D6
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
CYP2D6 catalyzes the hydroxylation of pregnenolone at 2-, 6-, 16-, and 21-positions (Hiroi et al. 2001). Pregnenolone is a steroid precursor to cortisol, dehydroepiandrosterone (DHEA), progesterone, and testosterone (Freeman et al. 2001). Pregnenolone can be converted to progesterone by 3β-hydroxysteroid dehydrogenase and Δ4–5 isomerase. In addition, pregnenolone can be converted to 17-hydroxy-pregnenolone by 17α-hydroxylase (CYP17A1), which is then converted to DHEA by desmolase. DHEA is the precursor of androstenedione.
Cannabis Use Treatment
Published in Jonathan C. Beazley, Stephanie Field, Cannabis on Campus, 2018
Jonathan C. Beazley, Stephanie Field
Unfortunately, some studies demonstrate high rates of relapse at six-month follow-ups for marijuana dependent individuals.61, 62 If medication-assisted treatment is to be a truly important adjunct, it must do more than just ease withdrawal, but also help individuals maintain significantly reduced use or abstinence long-term. In addition to the preliminary research from Nabilone trials, another study out of France suggested that the naturally occurring hormone pregnenolone might offer additional promise.63 They found rats who were given high amounts of THC also exhibited elevations of this hormone, suggesting pregnenolone may be an inherent, signal-activated, protective mechanism against over-intoxication, attenuating the effects of THC at the C1 receptors. Pregnenolone, in a future preparation might mitigate the psychoactive effects of marijuana, possibly extinguishing the urge to use. This action is already used in the substance abuse pharmacology world with naltrexone for alcohol dependence and Chantix and bupropion to interfere with the reward of tobacco.
Diurnal variation of metabolites in three individual participants
Published in Chronobiology International, 2019
Fangyi Gu, Elizabeth B. Klerman, Sungduk Kim, Steve Moore, Kai Yu, Paul S. Albert, Neil E Caporaso
In contrast, steroids peak in the morning. These molecules include cortisol, pregnenolone sulfate, and bilirubin. Cortisol is a hormone that increases in response to diverse physiologic stimuli, such as stress and low blood-glucose concentration. The morning rise in cortisol serves to increase blood sugar, elevate blood pressure, suppress the immune system, and to aid in macronutrient metabolism of fat, protein, and carbohydrates (Martin PA, 2003). Our results are consistent with previous reports in humans that blood cortisol has diurnal variation and peaks in the morning (Ang et al. 2012), (Martin 2003). Pregnenolone sulfate has cognitive, memory enhancing and antidepressant effects (Reddy 2010). Bilirubin is a product of heme catabolism, which has been suggested as a potential cellular antioxidant (Sedlak et al. 2009).
The future of type 1 cannabinoid receptor allosteric ligands
Published in Drug Metabolism Reviews, 2018
Mariam Alaverdashvili, Robert B. Laprairie
The sterol intermediate pregnenolone has been shown to attenuate the effects of THC in cell culture (Vallée et al. 2014). Pregnenolone acted consistent with a NAM for its effects of some aspects of CB1R agonism, such as inhibition of mitochondrial respiration and ERK1/2 phosphorylation, but not agonist equilibrium binding or cAMP modulation (Vallée et al. 2014). Further, inhibition of pregnenolone synthesis increases the potency and efficacy of THC in in vivo behavioral assays (Busquets-Garcia et al. 2017). The NAM effects of pregnenolone were not observed in later studies (Khajehali et al. 2015; Straiker et al. 2015; Gamage et al. 2014, 2017). Given their presence in the CB1R crystal structures solved to date (Hua et al. 2016, 2017; Shao et al. 2016), it is likely that cholesterol, and other sterols including pregnenolone, can play a modulatory role in CB1R pharmacology, but their precise mechanism(s) of action have yet to be determined.
Investigational drugs in early-stage clinical trials for autism spectrum disorder
Published in Expert Opinion on Investigational Drugs, 2019
Michael P. Hong, Craig A. Erickson
Pregnenolone is a neurosteroid metabolized to allopregnanolone, a biologic found to regulate activity at the GABA-A receptor [67]. Additionally, the sulfated form of pregnenolone (PregS) has been observed to alter cellular activity at the NMDA receptor [68]. In a small 12-week open-label trial, oral pregnenolone decreased irritability and lethargy and improved sensory deficits [69]. Trials with larger sample sizes and placebo-controlled studies are needed to further evaluate the efficacy and safety of pregnenolone in ASD.