Modulation of native and recombinant GABAA receptors by endogenous and synthetic neuroactive steroids

JJ Lambert, D Belelli, SC Harney, JA Peters… - Brain Research …, 2001 - Elsevier
Upon administration, certain pregnane steroids produce clear behavioural effects including,
anxiolysis, sedation, analgesia, anaesthesia and are anti-convulsant. This behavioural
profile is characteristic of compounds that act to enhance the actions of GABA acting at the
GABAA receptor. In agreement, numerous studies have now demonstrated these steroids to
be potent, positive allosteric modulators of the GABAA receptor. The pregnane steroids are
synthesized in the periphery by endocrine glands such as the adrenals and the ovaries, but …