gpr35 antagonist

ML-193 (CID 1261822) is a potent and selective GPR55 antagonist (IC50: 221 nM) with over 27-fold selectivity for GPR55 over GPR35, CB1, and CB2. It can ameliorate motor and sensorimotor deficits in Parkinson's disease (PD) rats.

CID1231538 is a potent GPR35 antagonist.

ML 145 is a selective and potent antagonist of human GPR35, with no significant activity against GPR35 in any of its immediate rodent homologs.ML 145 has potential anti-inflammatory activity for the study of immunoinflammation.ML 145 is a novel non-steroidal anti-inflammatory agent for the study of rheumatoid arthritis.

CID 2745687 is a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50 = 6.70. CID 2745687 cannot effectively antagonize the agonist effects of either Zaprinast or Cromolyn disodium at rodent ortholog of GPR35 in vitro[1]. However, CID 2745687 can reverse lodoxamide-mediated anti-fibrotic effects in mice in vivo[2].

Kynurenic acid (Quinurenic acid) is an endogenous tryptophan active metabolite, a triple antagonist of NMDA, glutamate, α7 nicotinic acetylcholine receptor, and an agonist of GPR35 CXCR8 with neuroprotective and anticonvulsant properties. It has neuroprotective and anticonvulsant properties and can be used to study neurodegeneration and metabolism-related diseases.

Kynurenic acid, an active metabolite of tryptophan, is synthesized through a kynurenine intermediate by kynurenine aminotransferases (KATs). It acts as an antagonist of both NMDA and AMPA receptors, as well as α7 nicotinic acetylcholine receptors (nAChRs; EC50s = 235, 101, and 7 µM, respectively), and functions as an agonist for the aryl hydrocarbon receptor (AhR) and G protein-coupled receptor 35 (GPR35; EC50s = 1.4 and 39 µM, respectively). In a neonatal rat model of cerebral hypoxic-ischemia, induced by carotid artery ligation, administration of kynurenic acid at 300 mg kg prevents weight loss in the lesioned hemisphere. Additionally, at concentrations of 1 and 5 mg ml, it protects against neurodegeneration in the rhabdomere of the eye in an Htt93QtransgenicDrosophila model of Huntington's disease. Elevated levels of kynurenic acid in the cerebrospinal fluid have been observed in patients with schizophrenia.

Kynurenic Acid-d5 is a deuterated compound of Kynurenic Acid. Kynurenic Acid has a CAS number of 492-27-3. Kynurenic acid, a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist.