Xanthine amine congener dihydrochloride (XAC dihydrochloride), a potent antagonist for both Adenosine A1 and A2 receptors, exhibits IC50 values of 1.8 nM for A1 and 114 nM for A2 receptors. Additionally, it functions as a convulsant agent in mouse models.
1,2,3,4,7,8-Hexachlorodibenzo-p-dioxin 是一种多氯二苯并二恶英 (PCDD) 同源物。在最高剂量 (10,000 μg kg) 下,该化合物可导致 H W 和 A 系大鼠肝脏苍白 (脂肪肝)、胃肠道出血和早期死亡。此外,1,2,3,4,7,8-Hexachlorodibenzo-p-dioxin 还会引起肝窦扩张,甚至导致 B 系大鼠严重紫癜。
Several different arachidonoyl amino acids, including N-arachidonoyl-L-alanine (NALA), have been isolated and characterized from bovine brain. The glycine congener (NAGly) was further characterized and found to suppress formalin-induced pain in rats. NALA may have activity at cannabinoid receptor and/or VR1, but has not been fully characterized to date.
TPU-0037A is an antibiotic and a congener of lydicamycin . It inhibits the growth of Gram-positive bacteria, including methicillin-resistant S. aureus (MRSA), B. subtilis, and M. luteus (MICs = 1.56-12.5 μg ml), but not Gram-negative E. coli, P. mirabilis, P. vulgaris, or P. aeruginosa strains (MICs = >50 μg ml).
Several different arachidonoyl amino acids, including N-arachidonoyl-3-hydroxy-γ-aminobutyric acid (NAG-3H-ABA), have been isolated and characterized from bovine brain. The glycine congener was further characterized and found to suppress formalin-induced pain in rats. NAG-3H-ABA was also found in rat brain by LC-MS techniques, but has not been fully characterized to date. Most arachidonoyl amino acids are poor ligands for the CB1 receptor.
CXCR4 antagonist 3 (compound 12a), an effective antagonist of CXCR4, exhibits an IC50 of 11 nM. It is a congener of TIQ15, showcasing exceptional properties such as CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. With its potential for research on the human immunodeficiency virus, CXCR4 antagonist 3 holds great promise [1].
2-Arachidonoyl glycerol (2-AG), a natural endocannabinoid ligand for the CB1 receptor, was isolated from porcine brain and characterized. Its congener, 2-linoleoyl glycerol (2-LG), which has a linoleoyl group instead of an arachidonoyl group, also exists alongside 2-AG in vivo. While 2-LG exhibits low intrinsic activity, it enhances the activity of 2-AG and other endocannabinoids through an entourage effect, attributed to the inhibition of breakdown and reuptake pathways that typically decrease endocannabinoid levels post-release.