congener

Xanthine amine congener dihydrochloride (XAC dihydrochloride), a potent antagonist for both Adenosine A1 and A2 receptors with IC50 values of 1.8 nM for A1 and 114 nM for A2, also functions as a convulsant agent in mouse models.

Xanthine amine congener trihydrochloride is a potent adenosine antagonist that reverses the reduction in urine flow, sodium excretion and heart rate produced by the adenosine agonist, N6-cyclohexyladenosine.

Adenosine amine congener (ADAC) (ADAC) is an agonist of selective A1 adenosine receptor,.

Xanthine amine congener (XAC) hydrochloride, a non-selective adenosine receptor antagonist, induces convulsions in mice.

Xanthine amine congener is an Adenosine receptor antagonist.

Tegafur (FT 207) is a congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme.

Cimetidine (SKF-92334) is a histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.

Nordihydrocapsaicin is an analog and congener of capsaicin, belonging to the capsaicinoid class of compounds found in Capsicum chili peppers.

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.

Demethyl bleomycin A2, a Bleomycin congener, exhibits DNA cleavage that is insensitive to the presence of 5-Methylcytidine [1].

M1 ligand 1 (compound 3b-b) is a N-desmethyl analog of the arecoline derivative, acting as a muscarinic acetylcholine receptor M1 ligand and usable as a PET (positron emission tomography) radiotracer [1].

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).

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].

Lankacyclinone C, a congener of lankacidin C devoid of the δ-lactone moiety, exhibits antitumor activity.

Ancitabine, a congener of cyterabine, is metabolized to cytarabine, thereby maintains a more constant antineoplastic action.

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.

8-iso PGF1α is an isoprostane that was first identified in human semen. It is a member of the isoprostane family, which are eicosanoids of non-cyclooxygenase origin. 8-iso PGF1α is present along with its 19-hydroxy congener at 5-10 μg/ml of seminal plasma.

Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine.

Lobophorin CR-2, a lobophorin congener, induces UPR-associated gene expression, inhibits oral squamous cell carcinoma cell growth, and causes UPR-dependent cell death in MEF cells [1].