Progesterone and progestins: Effects on brain, allopregnanolone and β-endorphin

Menstrual cycle and competitive bidding

“…Progesterone may have a sedating effect by acting as allosteric modulator of neurotransmitter receptors such as GABA-A (see Pluchino et al, 2006, van Broeckhoven et al, 2006. 11 Hence, one may reasonably expect that the use of hormonal contraceptives would reduce risk-taking, and thus increase bids on average.…”

Dydrogesterone increases allopregnanolone in selected brain areas and in serum of female rats

“…Allopregnanolone is a potent endogenous steroid that rapidly affects the excitability of neurons and glia cells through the direct modulation of the activity of g-aminobutyric acid A receptors (5, 6). Allopregnanolone exerts neuropharmacologic actions, with hypnotic/sedative, anxiolytic, anesthetic, and analgesic functions, and it enhances the myelination/remyelination process (7, 8).In addition, it has been demonstrated that chronic intraperitoneal treatment with progesterone or different progestins (medroxyprogesterone acetate [MPA], norethisterone acetate, desogestrel) as well as oral administration of active progestogens (MPA and drospirenone) directly influences the central nervous system's levels of b-endorphin in ovariectomized female rats (3,(9)(10)(11). Beta-endorphin exerts several behavioral, analgesic, thermoregulatory, and neuroendocrine properties (12).…”

“…These progestogens and their related metabolites may induce diverse functional response, depending on the chemical structure, their receptor-binding profile, the dose and the route of administration (1). Moreover, the interaction of synthetic progestins with metabolic pathways may induce divergent biological effects with respect to natural progesterone (2,3).…”

Progesterone increases the activity of glutamate transporter type 3 expressed in Xenopus oocytes

“…For example, progesterone has been shown to have analgesic and sedative properties (Frye et al, 2004;Van Broekhoven et al, 2006). Although an effect of progesterone on GABA receptors or opioid receptors has been proposed as the underlying mechanism (Dawson-Basoa and Gintzler, 1996;Pluchino et al, 2006), progesterone effects on glutamate signaling have recently received attention (Coronel et al, 2011;Ren et al, 2000). Additionally, progesterone and its metabolites have shown neuroprotective properties against traumatic brain injury (Stein, 2011).…”