Imidazopyridine

Sedatives

• Imidazopyridines:
• * Alpidem —an anxiolytic that was withdrawn from the market worldwide in 1995 due to hepatotoxicity.
• * DS-1—a GABA_A receptor positive allosteric modulator selective for the α₄β₃δ subtype, which is not targeted by other GABAergics such as benzodiazepines or other nonbenzodiazepines.
• * Necopidem—an anxiolytic. It has not found clinical use.
• * Saripidem—a sedative and anxiolytic. It is not used clinically.
• * TP-003—a subtype-selective partial agonist at GABA_A receptors, binding to GABA_A receptor complexes bearing either α₂, α₃ or α₅ subunits, but only showing significant efficacy at α₃.
• * Zolpidem —a widely used hypnotic. Generic versions are widely available.
• Imidazopyridines:
• * Bamaluzole—a GABA_A receptor-agonizing anticonvulsant that was never marketed.

  Antipsychotic

• Imidazopyridines:
• * Mosapramine —an atypical antipsychotic used in Japan.

  Gastrointestinal

• Imidazopyridines:
• * CJ-033466—an experimental gastroprokinetic acting as a selective 5-HT₄ serotonin receptor partial agonist.
• * Zolimidine—a gastroprotective agent.
• * Linaprazan—a potassium-competitive acid blocker which demonstrated similar efficacy as esomeprazole in healing and controlling symptoms of GERD patients with erosive esophagitis.
• * SCH28080—the prototypical potassium-competitive acid blocker which has not found clinical use because of liver toxicity in animal trials and elevated liver enzyme activity in the serum of human volunteers.
• Imidazopyridines:
• * Tenatoprazole—it blocks the gastric proton pump leading to decline of gastric acid production.

  Anti-inflammatories

• Imidazopyridines:
• * Miroprofen—a derivative of propionic acid.
• Imidazopyridines:
• * Telcagepant—a calcitonin gene-related peptide receptor antagonist which was in clinical trials as a remedy for migraine. Its development was terminated.

  Cardiovascular

• Imidazopyridines:
• * Olprinone —a cardiac stimulant.

  Bone

• Imidazopyridines:
• * Minodronic acid —a third-generation bisphosphonate used for the treatment of osteoporosis.

  Antineoplastic

• Imidazopyridines:
• * Fadrozole —an aromatase inhibitor.
• Imidazopyridines:
• * 3-Deazaneplanocin A—an S-adenosyl-L-homocysteine synthesis inhibitor and histone methyltransferase EZH2 inhibitor.

  Antiviral

• Imidazopyridines:
• * Tegobuvir - an allosteric, non-nucleoside hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitor targeting the thumb II allosteric site.