Direct effects of the anabolic/androgenic steroids, stanozolol and 17α-methyltestosterone, on benzodiazepine binding to the γ-aminobutyric acidA receptor

  title={Direct effects of the anabolic/androgenic steroids, stanozolol and 17$\alpha$-methyltestosterone, on benzodiazepine binding to the $\gamma$-aminobutyric acidA receptor},
  author={A. E. Tory Masonis and Michael P. McCarthy},
  journal={Neuroscience Letters},
Anabolic steroids induce region- and subunit-specific rapid modulation of GABA(A) receptor-mediated currents in the rat forebrain.
It is reported that in prepubertal female rats, three commonly abused AAS induced rapid and reversible modulation of GABAergic currents in neurons of two brain regions known to be critical for the expression of reproductive behaviors: the ventromedial nucleus of the hypothalamus and the medial preoptic area.


Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor.
Two metabolites of the steroid hormones progesterone and deoxycorticosterone are potent barbiturate-like ligands of the gamma-aminobutyric acid (GABA) receptor-chloride ion channel complex and potentiated the inhibitory actions of GABA in cultured rat hippocampal and spinal cord neurons, which may explain the ability of certain steroid hormones to rapidly alter neuronal excitability.
gamma-Aminobutyric acid (GABA)- and barbiturate-mediated 36Cl- uptake in rat brain synaptoneurosomes: evidence for rapid desensitization of the GABA receptor-coupled chloride ion channel.
The findings suggest that "desensitization" of the GABA receptor/Cl- ion channel may involve both the GABA and barbiturate recognition sites or a common effector component such as the ionophore itself.
Functional modulation of cerebral gamma-aminobutyric acidA receptor/benzodiazepine receptor/chloride ion channel complex with ethyl beta-carboline-3-carboxylate: presence of independent binding site for ethyl beta-carboline-3-carboxylate.
The present results suggest that the binding site for beta-CCE, which resides on GABAA receptor/benzodiazepine receptor/chloride ion channel complex, may be different from that for benzodiazepin.
Non-genomic and genomic effects of steroids on neural activity.
  • B. McEwen
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    Trends in pharmacological sciences
  • 1991
Psychiatric and medical effects of anabolic-androgenic steroid use. A controlled study of 160 athletes.
  • H. Pope, D. Katz
  • Medicine, Psychology
    Archives of general psychiatry
  • 1994
Major mood disturbances associated with anabolic-androgenic steroids may represent an important public health problem for athletes using steroids and sometimes for the victims of their irritability and aggression.
Hooked on hormones? An anabolic steroid addiction hypothesis.
It is concluded that a proportion of anabolic steroid abusers may develop a previously unrecognized sex steroid hormone-dependence disorder and that treatment should be based on research into steroid effects on opioid and aminergic neurotransmission systems and relapse prevention.
Psychological moods and subjectively perceived behavioral and somatic changes accompanying anabolic-androgenic steroid use
The data suggest that while perceived or actual psychological changes may occur in anabolic-androgenic steroid users, either the effects are too subtle or the inventories used were insensitive for detecting them.
Goodman and Gillman's The Pharmacological Basis of Therapeutics
The content of this edition has been significantly updated to include recently acquired experimental information, and has a well-written review of transmembrane signaling mechanisms, including G proteins and the protein kinases.