ChemInform Abstract: Discovery of Liver Selective Non-Steroidal Glucocorticoid Receptor Antagonist as Novel Antidiabetic Agents.

ChemInform ◽  
2013 ◽  
Vol 44 (4) ◽  
pp. no-no
Author(s):  
Kiran Shah ◽  
Dipam Patel ◽  
Pradip Jadav ◽  
Mubeen Sheikh ◽  
Kalapatapu V. V. M. Sairam ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Antidiabetic Agents

Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents

2012 ◽  
Vol 22 (18) ◽  
pp. 5857-5862 ◽  
Author(s):  
Kiran Shah ◽  
Dipam Patel ◽  
Pradip Jadav ◽  
Mubeen Sheikh ◽  
Kalapatapu V.V.M. Sairam ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Antidiabetic Agents

Effect of Glucocorticoid receptor antagonist administration in a Cushing's syndrome model rat

2019 ◽  
Author(s):  
Toshiro Seki ◽  
Atsushi Yasuda ◽  
Natsumi Kitajima ◽  
Masami Seki ◽  
Masayuki Oki ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Cushing’S Syndrome ◽  
Cushing's Syndrome

scholarly journals The influence of stress hormones and aggression on cooperative behaviour in subordinate meerkats

2017 ◽  
Vol 284 (1863) ◽  
pp. 20171248 ◽  
Author(s):  
Ben Dantzer ◽  
Ines Braga Goncalves ◽  
Helen C. Spence-Jones ◽  
Nigel C. Bennett ◽  
Michael Heistermann ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Treatment Effects ◽  
Stress Hormones ◽  
Cooperative Behaviour ◽  
Food Provisioning ◽  
Stress Hormone ◽  
Suricata Suricatta

In cooperative breeders, aggression from dominant breeders directed at subordinates may raise subordinate stress hormone (glucocorticoid) concentrations. This may benefit dominants by suppressing subordinate reproduction but it is uncertain whether aggression from dominants can elevate subordinate cooperative behaviour, or how resulting changes in subordinate glucocorticoid concentrations affect their cooperative behaviour. We show here that the effects of manipulating glucocorticoid concentrations in wild meerkats ( Suricata suricatta ) on cooperative behaviour varied between cooperative activities as well as between the sexes. Subordinates of both sexes treated with a glucocorticoid receptor antagonist (mifepristone) exhibited significantly more pup protection behaviour (babysitting) compared to those treated with glucocorticoids (cortisol) or controls. Females treated with mifepristone had a higher probability of exhibiting pup food provisioning (pup-feeding) compared to those treated with cortisol. In males, there were no treatment effects on the probability of pup-feeding, but those treated with cortisol gave a higher proportion of the food they found to pups than those treated with mifepristone. Using 19 years of behavioural data, we also show that dominant females did not increase the frequency with which they directed aggression at subordinates at times when the need for assistance was highest. Our results suggest that it is unlikely that dominant females manipulate the cooperative behaviour of subordinates through the effects of aggression on their glucocorticoid levels and that the function of aggression directed at subordinates is probably to reduce the probability they will breed.

Stress alters cutaneous permeability barrier homeostasis

2000 ◽  
Vol 278 (2) ◽  
pp. R367-R372 ◽  
Author(s):  
Mitsuhiro Denda ◽  
Toru Tsuchiya ◽  
Peter M. Elias ◽  
Kenneth R. Feingold
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Psychological Stress ◽  
Skin Disease ◽  
Barrier Function ◽  
Plasma Corticosterone ◽  
Permeability Barrier ◽  
Hairless Mice ◽  
Ru 486 ◽  
Kinetics Of

Recent studies have shown that psychological stress can influence cutaneous barrier function, suggesting that this form of stress could trigger or aggravate skin disease. In the present study, we demonstrate that transfer of hairless mice to a different cage delays barrier recovery rates. Pretreatment with a phenothiazine sedative, chlorpromazine, before transfer of animals restored the kinetics of barrier recovery toward normal, suggesting that psychological stress is the basis for this alteration in barrier homeostasis. To determine the mechanism linking psychological stress to altered barrier recovery, we first demonstrated that plasma corticosterone levels increase markedly after transfer of animals to new cages and that pretreatment with chlorpromazine blocks this increase. Second, we demonstrated that the systemic administration of corticosterone delays barrier recovery. Finally, we demonstrated that pretreatment with the glucocorticoid receptor antagonist RU-486 blocks the delay in barrier recovery produced by systemic corticosterone, change of cage, or immobilization. These results suggest that psychological stress stimulates increased production of glucocorticoids, which, in turn, adversely affects permeability barrier homeostasis.

scholarly journals Selective Glucocorticoid Receptor Antagonist CORT125281 Activates Brown Adipose Tissue and Alters Lipid Distribution in Male Mice

Endocrinology ◽  
2017 ◽  
Vol 159 (1) ◽  
pp. 535-546 ◽  
Author(s):  
Jan Kroon ◽  
Lisa L Koorneef ◽  
Jose K van den Heuvel ◽  
Cristy R C Verzijl ◽  
Nienke M van de Velde ◽  
...  
Keyword(s):  
Adipose Tissue ◽  
Glucocorticoid Receptor ◽  
Brown Adipose Tissue ◽  
Receptor Antagonist ◽  
Male Mice ◽  
Lipid Distribution ◽  
Brown Adipose

scholarly journals Hypothalamic-Pituitary-Adrenal Axis Activity of Newborn Mice Rapidly Desensitizes to Repeated Maternal Absence but Becomes Highly Responsive to Novelty

Endocrinology ◽  
2008 ◽  
Vol 149 (12) ◽  
pp. 6366-6377 ◽  
Author(s):  
L. Enthoven ◽  
M. S. Oitzl ◽  
N. Koning ◽  
M. van der Mark ◽  
E. R. de Kloet
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Hpa Axis ◽  
Mineralocorticoid Receptor ◽  
Maternal Separation ◽  
Mineralocorticoid Receptor Antagonist ◽  
Newborn Mice ◽  
Hypothalamic Pituitary Adrenal ◽  
The Third ◽  
Corticosterone Response

In CD1 mice we investigated the hypothalamic-pituitary-adrenal (HPA) axis response to maternal separation for 8 h daily from postnatal d 3 to 5. At d 3 a slow separation-induced corticosterone response developed that peaked after 8 h, and the pups became responsive to stressors. On the second and third day, the response to 8 h separation rapidly attenuated, whereas the response to novelty did not, a pattern reflected by the hypothalamic c-fos mRNA response. If maternal separation and exposure to novelty were combined, then after the third such daily exposure, the sensitivity to the stressor was further enhanced. Meanwhile, basal corticosterone and ACTH levels were persistently suppressed 16 h after pups were reunited with their mothers. To explain the HPA axis desensitization after repeated separation, we found that circulating ghrelin levels increased and glucose levels decreased after all periods of maternal separation, ruling out a role of altered metabolism. Glucocorticoid feedback was not involved either because a glucocorticoid receptor antagonist amplified the corticosterone response after the first but became ineffective after the third separation. In contrast, a mineralocorticoid receptor antagonist decreased and increased corticosterone levels after the first and third period of separation, respectively. In conclusion, the newborn’s HPA axis readily desensitizes to repeated daily maternal separation, but continues to respond to novelty in a manner influenced by a central mineralocorticoid receptor- rather than glucocorticoid receptor-mediated mechanism.

Effect of the Glucocorticoid Receptor Antagonist Org 34850 on Basal and Stress-Induced Corticosterone Secretion

2007 ◽  
Vol 19 (11) ◽  
pp. 891-900 ◽  
Author(s):  
F. Spiga ◽  
L. R. Harrison ◽  
S. A. Wood ◽  
H. C. Atkinson ◽  
C. P. MacSweeney ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Corticosterone Secretion

scholarly journals The selective glucocorticoid receptor antagonist CORT 108297 decreases neuroendocrine stress responses and immobility in the forced swim test

2014 ◽  
Vol 65 (4) ◽  
pp. 363-371 ◽  
Author(s):  
Matia B. Solomon ◽  
Aynara C. Wulsin ◽  
Taylor Rice ◽  
Dayna Wick ◽  
Brent Myers ◽  
...  
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Antagonist ◽  
Stress Responses ◽  
Forced Swim Test ◽  
Swim Test ◽  
Forced Swim
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