Antagonist, Partial Agonist, and Full Agonist Imidazo[1,5-a]quinoxaline Amides and Carbamates Acting through the GABAA/Benzodiazepine Receptor. Ruth E. TenBrink,Wha B. Im,Vimala H. Sethy,Andrew H. Tang,Don B. Carter. Journal of Medicinal Chemistry . 1994...
Since cAMP signaling regulates cell proliferation and differentiation, abnormal cAMP biogenesis is involved in tumorigenesis, a complex disease resulting from diverse environmental and genetic factors [11]. cAMP has a significant impact on both cancer cells and the tumor microenvironment (TME). Cytokines,...
PPARγ partial agonist like balaglitazone has been demonstrated clinically exerting good antidiabetic action with reduced adverse effects that are associated with PPARγ full agonist, pioglitazone (Henriksen et al., 2011). In an effort to identify novel PPARγ ligands with an improved pharmacological...
Opioid-receptor binding and the opioid-mediated stimulation of low K m GTPase and inhibition of adenylate cyclase were studied in membranes derived from NG 108-15 cells pretreated with either the opioid peptide [ d-Ala 2, d-Leu 5]enkephalin (DADLE) or morphine. Pretreatment with DADLE resulted...
Other notable downstream substrates whose activation states are modified by AKT include IκB kinase (IKK) [82], mouse double minute 2 homolog (Mdm2) [83,84], which promotes the ubiquitination and degradation of p53, the pro-apoptotic proteins BCL-2 associated agonist of cell death (Bad) and...
Nabilone is a partial agonist of cannabinoid receptor 1 (CB1) and CB2 in the brain and in peripheral tissues, and it has been reported to provide effective treatment for agitation in patients with AD [78]. A phase 3 trial (NCT04516057) was started in February 2021 to investigate whether ...
This concept was then improved on by evidence of the neuroactivity of KP metabolites; for example, Quin, an excitotoxic agonist of the N-methyl-D-aspartic acid receptor (NMDAR) [52], is involved in at least nine mechanisms of neurotoxicity, including ROS production, BBB damage, cytoskeleton ...
[184,185]. The activity of DDA in inducing lethal autophagy contributes to its anti-leukemic effects on AML cells in vitro and in vivo. DDA, as a partial agonist for liver-X-receptor triggers Nur77- and NOR1-dependent autophagy, which is associated with increased LC3-II expression in AML...
The primary bile acid CDCA is the strongest agonist for FXR followed by CA, the secondary bile acid DCA, and LCA [77], while the murine taurine-conjugated bile acids TMCA antagonize FXR [78]. Activation of FXR was shown to improve hyperlipidemia and hyperglycemia in db/db mice by ...
Dhalla, Arvinder et al., “Antilipolytic Activity of a Novel partial A(1) Adenosine Receptor Agonist Devoid of Cardiovascular Effects: Comparison with Nicotinic Acid”, Journal of Pharmacology and Experimental Therapeutics, vol. 321, No. 1 Apr. 2007, pp. 327-333. Morrison, Christopher et al...