Selective activation of estrogen receptors, ERα and GPER-1, rapidly decreases food intake in female rats

Butler, Michael J.; Hildebrandt, Ryan P.; Eckel, Lisa A.

doi:10.1016/j.yhbeh.2018.05.018

Cited by 22 publications

(18 citation statements)

References 47 publications

(79 reference statements)

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“…GPER-mediated rapid signaling is demonstrated in tissues such as blood vessels, where it induces vasodilation via nitric oxide (NO) and cAMP signaling [20] and impacts calcium mobilization [25]. GPER activation also increases mitochondrial calcium retention in the heart within minutes [26] and decreases central control of food intake within an hour [27], both of which demonstrate the importance of this non-genomic pathway. The greater variability and tissue specificity for ESR1 and ESR2 may be important for regulating the large number of genes that are important for growth and reproduction.…”

Section: Discussionmentioning

confidence: 99%

Estrogen receptor profiles across tissues from male and female Rattus norvegicus

et al. 2019

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BackgroundEstrogen is formed by the enzyme aromatase (CYP19A1) and signals via three identified receptors ERα (ESR1), ERß (ESR2), and the G protein-coupled estrogen receptor (GPER). Understanding the relative contribution of each receptor to estrogenic signaling may elucidate the disparate effects of this sex hormone across tissues, and recent developments in PCR technology allow absolute quantification and direct comparison of multiple targets. We hypothesized that this approach would reveal tissue- and sex-specific differences in estrogen receptor mRNA.MethodsESR1, ESR2, GPER, and CYP19A1 were measured in four cardiovascular tissues (heart, aorta, kidney, and adrenal gland), three brain areas (somatosensory cortex, hippocampus, and prefrontal cortex), and reproductive tissues (ovaries, mammary gland, uterus, testes) from six male and six female adult Sprague-Dawley rats.ResultsGPER mRNA expression was relatively stable across all tissues in both sexes, ranging from 5.49 to 113 copies/ng RNA, a 21-fold difference. In contrast, ESR1/ESR2 were variable across tissues although similar within an organ system. ESR1 ranged from 4.46 to 614 copies/ng RNA (138-fold difference) while ESR2 ranged from 0.154 to 83.1 copies/ng RNA (540-fold). Significant sex differences were broadly absent except for renal ESR1 (female 206 vs. male 614 copies/ng RNA, P < 0.0001) and GPER (62.0 vs. 30.2 copies/ng RNA, P < 0.05) as well as gonadal GPER (5.49 vs. 47.5 copies/ng RNA, P < 0.01), ESR2 (83.1 vs. 0.299 copies/ng RNA, P < 0.01), and CYP19A1 (322 vs. 7.18 copies/ng RNA, P < 0.01). Cardiovascular tissues showed a predominance of ESR1, followed by GPER. In contrast, GPER was the predominant transcript in the brain with similarly low levels of ESR1 and ESR2. CYP19A1 was detected at very low levels except for reproductive tissues and the hippocampus.ConclusionWhile the data indicates a lack of sex differences in most tissues, significant differences were found in the range of receptor gene expression across tissues as well as in the receptor profile between organ systems. The data provide a guide for future studies by establishing estrogen receptor expression across multiple tissues using absolute PCR quantification. This knowledge on tissue-specific estrogen receptor profiles will aid the development of hormonal therapies that elicit beneficial effects in specific tissues.

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Section: Discussionmentioning

confidence: 99%

Estrogen receptor profiles across tissues from male and female Rattus norvegicus

et al. 2019

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“…For all experiments, animals had free access to powdered rat chow (5001 Rodent Diet, LabDiet, 3.36 kcal·g −1 ; 28.5% protein, 13.5% fat, 58.0% carbohydrate) and tap water unless otherwise specified. Power analyses ( α = .05, 1‐β = .95) using an estimated effect size of 1 (based on previous studies, Butler, Hildebrandt, & Eckel, ) indicated a minimum necessary sample size of seven to eight animals per treatment group for the experiments described below.…”

Section: Methodsmentioning

confidence: 99%

The novel cannabinoid CB₁ receptor agonist AM11101 increases food intake in female rats

Ogden

Malamas

Makriyannis

et al. 2019

British J Pharmacology

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Background and Purpose Δ9‐tetrahydrocannabinol (THC) acts via cannabinoid CB1 receptors to increase feeding. Here, we assessed the orexigenic effect of AM11101, a novel CB1 receptor agonist designed to have a more favourable pharmacodynamic profile than THC. Experimental Approach The acute, orexigenic effects of AM11101 and THC were compared in female rats. Food intake and meal patterns were also examined following once daily treatment with AM11101 and THC for 7 days. Key Results AM11101 (0.01–0.1 mg·kg−1) increased food intake during the first hour following both acute and chronic treatments in pre‐fed and freely feeding animals. This orexigenic effect persisted for up to 4 hr, with no compensatory decrease in feeding during the subsequent 4–22 hr. THC (1 mg·kg−1) increased 1‐hr food intake in pre‐fed animals, but was less reliable than AM11101 in increasing 1‐hr food intake in freely feeding animals following both acute and chronic administration. The orexigenic effect of both compounds was due to an increase in meal size, not meal number. Conclusions and Implications Our study provides the first demonstration that AM11101 increases short‐term food intake via a selective increase in meal size. AM11101 promotes a more reliable orexigenic effect than THC in freely feeding animals, with no subsequent compensatory decrease in feeding. AM11101 may offer a greater efficacy than THC and its congeners in stimulating food intake in underweight clinical populations.

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“…Estradiol has also been shown to enhance the acquisition of LiCl‐induced taste aversion in castrated male rats, possibly due to estradiol's illness inducing properties. In addition, the formation of conditioned taste aversion and reduction of food intake seen after administration of agonists for ERα, ERβ and GPER‐1 is likely associated with the nausea and potentially disgust related responses elicited by estrogens, . These actions may also be related to ERs association with OT which is involved in the elicitation of anticipatory disgust …”

Section: Neurobiology Of Disgust and Pathogen/toxin Avoidancementioning

confidence: 99%

“…In addition, the formation of conditioned taste aversion and reduction of food intake seen after administration of agonists for ERα, ERβ and GPER-1 is likely associated with the nausea and potentially disgust related responses elicited by estrogens,. 111,112 These actions may also be related to ERs association with OT which is involved in the elicitation of anticipatory disgust. 78 Oxytocin has been implicated in the expression of the effects of ERs on social recognition and the display of the disgust and avoidance responses to pathogen threat.…”

Section: Estrogens Disgust and Pathogen/toxin Avoidancementioning

confidence: 99%

Social neuroscience of disgust

Kavaliers

Ossenkopp

Choleris

2018

Genes Brain and Behavior

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Disgust can be thought of as an affective system that has evolved to detect signs of pathogens, parasite and toxins as well as to stimulate behaviors that reduce the risk of their acquisition. Disgust incorporates social cognitive mechanisms to regulate exposure to and, or anticipate and avoid exposure to pathogens and toxins. Social cognition entails the acquisition of social information about others (ie, social recognition) and from others (ie, social learning). This involves recognizing and assessing other individuals and the pathogen/parasite/contamination/toxin threat they pose and deciding about when and how to interact with and, or avoid them. Social cognition provides a frame-work for examining the expression of disgust and the associated neurobiological mechanisms. Here, we briefly consider the relations between social cognition and pathogen/parasite/toxin avoidance behaviors. We briefly discuss aspects of: (1) the odor mediated social recognition of actual and potentially infected individuals and the impact of parasite/pathogen threat on disgust mate and social partner choice; (2) the roles of "out-groups" (strangers, unfamiliar individuals) and "in-groups" (familiar individuals) in the expression of disgust and pathogen avoidance behaviors; (3) individual and social learning of disgust and empathy for disgust; (4) toxin elicited disgust and anticipatory disgust; (5) the neurobiological mechanisms, and in particular the roles of the nonapeptide, oxytocin and estrogenic mechanism associated with social cognition and the expression of disgust. These findings on the social neuroscience of disgust have a direct bearing on our understanding of the roles of disgust in shaping human and nonhuman social behavior.

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Selective activation of estrogen receptors, ERα and GPER-1, rapidly decreases food intake in female rats

Cited by 22 publications

References 47 publications

Estrogen receptor profiles across tissues from male and female Rattus norvegicus

Estrogen receptor profiles across tissues from male and female Rattus norvegicus

The novel cannabinoid CB₁ receptor agonist AM11101 increases food intake in female rats

Social neuroscience of disgust

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Selective activation of estrogen receptors, ERα and GPER-1, rapidly decreases food intake in female rats

Cited by 22 publications

References 47 publications

Estrogen receptor profiles across tissues from male and female Rattus norvegicus

Estrogen receptor profiles across tissues from male and female Rattus norvegicus

The novel cannabinoid CB1 receptor agonist AM11101 increases food intake in female rats

Social neuroscience of disgust

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Product

Resources

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The novel cannabinoid CB₁ receptor agonist AM11101 increases food intake in female rats