SEX DIFFERENCES IN THE EFFECT OF ETHANOL INJECTION AND CONSUMPTION ON BRAIN ALLOPREGNANOLONE LEVELS IN C57BL/6 MICE D. A. FINN, a,b,c * R. S. SINNOTT, a1 M. M. FORD, a S. L. LONG, a M. A. TANCHUCK a AND T. J. PHILLIPS a,b,c a Department of Behavioral Neuroscience, Oregon Health & Science University, Portland, OR 97239, USA b Portland Alcohol Research Center, Portland, OR, USA c Department of Veterans Affairs Medical Center, 3710 SW U.S. Vet- erans Hospital Road, Portland, OR 97239, USA Abstract—The pharmacological profile of allopregnanolone, a neuroactive steroid that is a potent positive modulator of -aminobutyric acid A (GABA A ) receptors, is similar to that of ethanol. Recent findings indicate that acute injection of eth- anol increased endogenous allopregnanolone to pharmaco- logically relevant concentrations in male rats. However, there are no comparable data in mice, nor has the effect of ethanol drinking on endogenous allopregnanolone levels been inves- tigated. Therefore, the present studies measured the effect of ethanol drinking and injection on allopregnanolone levels in male and female C57BL/6 mice. One group was given 17 days of 2-h limited access to a 10% v/v ethanol solution in a preference-drinking paradigm, while another group had ac- cess to water only. The ethanol dose consumed in 2 h ex- ceeded 2 g/kg. Then, separate groups of mice were injected with either 2 g/kg ethanol or saline. Mice were killed 30 min after the 2-h drinking session or injection. Blood ethanol concentration was significantly higher in the ethanol-injected versus ethanol-drinking groups, even though the dose was similar. Consumption of ethanol significantly increased brain allopregnanolone levels in male but not female mice, com- pared with animals drinking water, but did not alter plasma corticosterone levels. In contrast, injection of ethanol did not significantly alter brain allopregnanolone levels in male or female mice and only significantly increased plasma cortico- sterone levels in the male mice, when compared with saline- injected animals. The sex differences in the effect of ethanol administration on endogenous allopregnanolone levels suggest that the hormonal milieu may impact ethanol’s effect on GABAergic neurosteroids. Importantly, these data are the first to report the effect of ethanol drinking on allopregnanolone levels and indicate that ethanol consumption and ethanol injection can produce physiologically relevant allopregnanolone levels in male mice. These results have important implications for studies investigating the potential role of endogenous allo- pregnanolone levels in modulating susceptibility to ethanol abuse. © 2004 IBRO. Published by Elsevier Ltd. All rights reserved. Key words: neurosteroid, alcohol drinking, alcohol injection, male, female, corticosterone. Rapid membrane effects of steroid hormones provide a mechanism by which steroids can influence brain function and behavior, in addition to their classical genomic actions. Within the last 20 years, some of these rapid non-genomic actions of steroid hormones have been demonstrated to occur via an interaction with ligand-gated ion channels, such as the -aminobutyric acid A (GABA A ) receptor (see review by Brann et al., 1995). For example, the progester- one derivative allopregnanolone (ALLOP, 3-hydroxy-5- pregnan-20-one) is a very potent positive modulator of GABA A receptors, and exogenous administration pro- duces anxiolytic, sedative, anticonvulsant and locomotor stimulant effects in animals (for reviews, see Paul and Purdy, 1992; Lambert et al., 1995; Gasior et al., 1999). It has also been demonstrated that stress, estrous cycle and pregnancy can increase endogenous ALLOP to levels that are physiologically relevant (see Paul and Purdy, 1992; Barbaccia et al., 1994, 1996; Concas et al., 1998). These findings suggest that fluctuations in endogenous levels of a neuroactive steroid such as ALLOP could modify the functioning of central GABA A receptors in vivo. Therefore, ALLOP may represent a physiologically significant neuro- modulator. The pharmacological profile of ALLOP is similar to that of ethanol (EtOH). While the effects of ALLOP appear to be primarily mediated via its interaction with GABA A recep- tors, EtOH interacts with multiple receptor systems, with one effect being to potentiate GABA A receptor function (see review by Grobin et al., 1998; Morrow et al., 2001). It has been suggested that certain behavioral effects of EtOH and neuroactive steroids may share a GABAergic mechanism (Grobin et al., 1998; Morrow et al., 2001). Recent findings indicate that acute administration of AL- LOP increased EtOH-reinforced operant responding and established EtOH drinking behavior in male rodents (Janak et al., 1998; Morrow et al., 2001; Sinnott et al., 2002). Sensitivity to the modulatory effect of ALLOP on EtOH drinking behavior in male rodents differed, depending on the concentration of the EtOH solution (Sinnott et al., 2002) and whether or not the animals were physically dependent (Morrow et al., 2001), suggesting that increases or de- 1 Present address: CROET (L-606), Oregon Health & Science Univer- sity, Portland, OR 97239, USA. *Correspondence to: D. A. Finn, Department of Veterans Affairs Med- ical Center, 3710 SW U.S. Veterans Hospital Road, Portland, OR 97239, USA. Tel: +1-503-721-7984; fax: +1-503-273-5351. E-mail address: finnd@ohsu.edu (D. A. Finn). Abbreviations: ALLOP, allopregnanolone (3-hydroxy-5-pregnan- 20-one); B6, C57BL/6; BEC, blood ethanol concentration; CORT, corticosterone; EtOH, ethanol; GABA A , -aminobutyric acid A ; HPA, hypothalamic–pituitary–adrenal; RIA, radioimmunoassay. Neuroscience 123 (2004) 813– 819 0306-4522/04$30.00+0.00 © 2004 IBRO. Published by Elsevier Ltd. All rights reserved. doi:10.1016/j.neuroscience.2003.11.017 813