1. GPCR/G Protein
    Neuronal Signaling
    Membrane Transporter/Ion Channel
    Metabolic Enzyme/Protease
    Autophagy
  2. Cannabinoid Receptor
    TRP Channel
    Endogenous Metabolite
    Autophagy
  3. Pregnenolone

Pregnenolone (Synonyms: 3β-Hydroxy-5-pregnen-20-one)

Cat. No.: HY-B0151 Purity: 98.05%
Handling Instructions

Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.

For research use only. We do not sell to patients.

Pregnenolone Chemical Structure

Pregnenolone Chemical Structure

CAS No. : 145-13-1

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Description

Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].

IC50 & Target[1]

CB1

 

Human Endogenous Metabolite

 

In Vitro

CB1 receptor stimulation increases brain Pregnenolone levels, which in turn exerts a negative feedback on the activity of the CB1 receptor antagonizing most of the known behavioral and somatic effects of THC. Pregnenolone likely acts as a signaling-specific negative allosteric modulator binding to a site distinct from that occupied by orthosteric ligands. Pregnenolone does not modify agonist binding but only agonist efficacy[1].
The effect of THC is significantly attenuated when slices are pre-treated with Pregnenolone 100 nM (15.1±1.8 % of inhibition). These effects are likely due to a pre-synaptic action of Pregnenolone. Thus, Pregnenolone blocks the increase in paired-pulse ratio (PPR) induced by THC but does not modify either the amplitude or the decay time of miniature EPSC (mEPSC)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

316.48

Formula

C₂₁H₃₂O₂

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (78.99 mM; ultrasonic and warming and heat to 60°C)

H2O : 0.1 mg/mL (0.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1598 mL 15.7988 mL 31.5976 mL
5 mM 0.6320 mL 3.1598 mL 6.3195 mL
10 mM 0.3160 mL 1.5799 mL 3.1598 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 1.25 mg/mL (3.95 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice and Rats[1]
Adult male Wistar rats (weighing 320-340g), Sprague Dawley male rats (weighing 330-350g), C57BL/6N mice (2-3 months) and CD1 mice (weighing 25-30 g at the beginning of the experiments) are used. Pregnenolone is injected subcutaneously (sc). The injection volumes are 1 mL/kg of body weight for rats and 10 mL/kg for mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.05%

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