Topigen Pharmaceuticals, Respiratory Research

March 2, 2021

Synthesis and Assessment of fused β-carboline derivatives as Kappa Opioid Receptor agonist

The synthesis of 5-formyl-6-aryl-6H-indolo[3,2,1-de][1,5] naphthyridine-2-carboxylates by way of response between 1-formyl-9H-b-carbolines and cinnamaldehydes within the presence of pyrrolidine in water beneath microwave irradiation is described. Pharmacophoric modification of the formyl group provided a number of new fused-b-carboline derivatives which have been investigated for his or her k-opioid receptor (KOR) agonistic exercise. Two compounds 4a and

March 2, 2021

Development of hMC1R Selective Small Agonists for Sunless Tanning and Prevention of Genotoxicity of UV in Melanocytes

Activation of the human melanocortin 1 receptor (hMC1R) expressed on melanocytes by α-melanocortin (α-MSH) performs a central function in regulating human pigmentation, and lowering the genotoxicity of ultraviolet radiation (UV) by activating DNA restore and antioxidant defenses. In the direction of growth of a hMC1R-targeted photoprotection technique we designed tetra- and tripeptide agonists with modifications

March 2, 2021

Adenosine A3 agonists reverse neuropathic pain via T cell-mediated production of IL-10

The A3 adenosine receptor (A3AR) has emerged as a therapeutic goal with A3AR agonists to deal with the worldwide problem of neuropathic ache; investigation into their mode of motion is important for ongoing medical growth. A3ARs on immune cells, and their activation throughout pathology, modulates cytokine launch. Thus, immune cells as a mobile substrate for

March 2, 2021

Discovery of ACH-000143: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats

The modulation of melatonin signaling in peripheral tissues holds promise for treating metabolic ailments like weight problems, diabetes, and nonalcoholic steatohepatitis. Right here, a number of benzimidazole derivatives have been recognized as novel agonists of the melatonin receptors MT1 and MT2. The lead compounds 10b, 15a, and 19a demonstrated subnanomolar efficiency at MT1/MT2 receptors, excessive

March 2, 2021

Anti-PTSD Effects of Hypidone Hydrochloride (YL-0919): A Novel Combined Selective 5-HT Reuptake Inhibitor/5-HT 1A Receptor Partial Agonist/5-HT 6 Receptor Full Agonist

Posttraumatic stress dysfunction (PTSD) is a debilitating trauma and stressor-related dysfunction that has develop into a serious neuropsychiatric downside, resulting in substantial disruptions in particular person well being and societal prices. Our earlier research have demonstrated that hypidone hydrochloride (YL-0919), a novel mixed selective 5-HT reuptake inhibitor/5-HT1A receptor partial agonist/5-HT6 receptor full agonist, exerts notable antidepressant- and

March 2, 2021

Design and Immunological Evaluation of a Hybrid Peptide as a Potent TLR2 Agonist by Structure-Based Virtual Screening

Immunity is a flexible defensive response that’s concerned in defending in opposition to illness by figuring out and destroying self and non-self dangerous substances. As a state of non permanent or everlasting immune dysfunction, immunosuppression could make an organism extra inclined to an infection, organ harm, and most cancers attributable to harm to the immune

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Blog

Synthesis and Assessment of fused β-carboline derivatives as Kappa Opioid Receptor agonist

Development of hMC1R Selective Small Agonists for Sunless Tanning and Prevention of Genotoxicity of UV in Melanocytes

Adenosine A3 agonists reverse neuropathic pain via T cell-mediated production of IL-10

Discovery of ACH-000143: A Novel Potent and Peripherally Preferred Melatonin Receptor Agonist that Reduces Liver Triglycerides and Steatosis in Diet-Induced Obese Rats

Anti-PTSD Effects of Hypidone Hydrochloride (YL-0919): A Novel Combined Selective 5-HT Reuptake Inhibitor/5-HT 1A Receptor Partial Agonist/5-HT 6 Receptor Full Agonist

Design and Immunological Evaluation of a Hybrid Peptide as a Potent TLR2 Agonist by Structure-Based Virtual Screening