Abstract Objective: Cannabinoids are a class of compounds that have the ability to activate two specific receptor subtypes, the cannabinoid CB1 and CB2 receptors. CB1 receptor is a G-protein-coupled receptor that is linked to the signal transduction pathways. The cumulative effects of this receptor have important implications in the control of cell survival and cell death having the potential to regulate tumor cell growth. In this connection, interest has been focused on factors such as sex steroid hormones, which regulate CB1 receptor expression. The aim of this study was to investigate the effects of 17beta-estradiol exposure on the CB1 receptor gene and its protein expression...

An anecdotal report of gynecomastia in chronic cannabis smokers [1] stimulated research into the effect of cannabis on male hormones [2,3]. A causal association between cannabis and gynecomastia was hypothesized based on the structural similarity of tetrahydrocannabinol (THC) and estradiol. Moreover, tetrahydrocannabinol was shown to directly stimulate development in rat breast tissue [4]. Although laboratory investigations on human subjects provided conflicting results regarding the effects of cannabis use on testosterone levels [2,3], one study failed to demonstrate any influence of intensive cannabis use on prolactin levels [2]. The present report is a case-control study of gynecomastia in a military population-US Army soldiers in Nuremberg,...

Crude marijuana extract competed with estradiol for binding to the estrogen receptor of rat uterine cytosol. Condensed manjuana smoke also competed with estradiol for its receptor. Pure 9-tetrahydrocannabinol, however, did not interact with the estrogen receptor. Ten i9-tetrahydrocannabinol metabolites also failed to compete with estradiol for its receptor. Of several other common cannabinoids tested, only cannabidiol showed any estrogen receptor binding. This was evident only at very high concentrations of cannabidiol. Apigenin, the aglycone of a flavinoid phytoestrogen found in cannabis, displayed high affinity for the estrogen receptor. To assess the biological significance of these receptor data, estrogen activity was measured in vivo with...

Aims/hypothesis: We examined the presence of functional cannabinoid receptors 1 and 2 (CB1, CB2) in isolated human islets, phenotyped the cells producing cannabinoid receptors and analysed the actions of selective cannabinoid receptor agonists on insulin, glucagon and somatostatin secretion in vitro. We also described the localisation on islet cells of: (1) the endocannabinoid-producing enzymes Nacyl-phosphatidyl ethanolamine-hydrolysing phospholipase D and diacylglycerol lipase; and (2) the endocannabinoiddegrading enzymes fatty acid amidohydrolase and monoacyl glycerol lipase. Methods: Real-time PCR, western blotting and immunocytochemistry were used to analyse the presence of endocannabinoid-related proteins and genes. Static secretion experiments were used to examine the effects of activating CB1 or...

The effects of delta9-tetrahydrocannabinol (THC) and cannabidiol (CBD) on hydroxylation of estradiol and testosterone in rat liver microsomes were investigated. Acute and chronic treatment of male and female rats with either cannabinoid, 2 or 10 mg/kg, significantly elevated steroid hydroxylase activity. Acute administration of THC or CBD, 10 mg/kg, evoked no detectable changes in cytochrome P-450 levels, but a significant decrease in those of cytochrome b5. Chronic administration of THC or CBD, 2 mg/kg, decreased levels of cytochrome P-450, whereas cytochrome b5 levels appeared normal. Acute doses of THC or CBD at 10 mg/kg significantly depressed testosterone formation in testis microsomes. Chronic THC, 2...

During the last few years, the endocannabinoid system has emerged as a highly relevant topic in the scientific community. Many different regulatory actions have been attributed to endocannabinoids, and their involvement in several pathophysiological conditions is under intense scrutiny. Cannabinoid receptors, named CB1 receptor and CB2 receptor, first discovered as the molecular targets of the psychotropic component of the plant Cannabis sativa, participate in the physiological modulation of many central and peripheral functions. CB2 receptor is mainly expressed in immune cells, whereas CB1 receptor is the most abundant G protein-coupled receptor expressed in the brain. CB1 receptor is expressed in the hypothalamus and the...