Results 61 to 70 of about 13,221 (154)
Synthesis of the calcilytic ligand NPS 2143
Beilstein Journal of Organic Chemistry, 2013 (R)-3 (NPS 2143) is a negative allosteric modulator of the human calcium-sensing receptor (CaSR) and as such represents an important pharmacological tool compound for studying the CaSR.
Henrik Johansson +4 more
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Moleculesμ-opioid receptor ligands such as morphine and fentanyl are the most known and potent painkillers. However, the severe side effects seen with their use significantly limit their widespread use.
Dominik Straszak +7 more
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International Journal for Parasitology: Drugs and Drug Resistance, 2016 Soil-transmitted helminth infections in humans and livestock cause significant debility, reduced productivity and economic losses globally. There are a limited number of effective anthelmintic drugs available for treating helminths infections, and their ...
Fudan Zheng +4 more
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SAG1.3-derived Frizzled-targeting negative allosteric modulators
Abstract Exaggerated Wingless/Int1 (WNT)/Frizzled (FZD) signaling contributes to pathologies including fibrosis and different forms of cancers. Thus, targeting FZDs as WNT receptors for therapeutic purposes constitutes a promising intervention if the imminent risk of unwanted side effects caused by the involvement of WNT/FZD signaling in stem ...
Gunnar Schulte +14 more
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Sodium functions as a negative allosteric modulator of the oxytocin receptor
Biochimica et Biophysica Acta (BBA) - Biomembranes, 2018 The oxytocin receptor, a class A G protein coupled receptor (GPCR), is essentially involved in the physiology of reproduction. Two parameters are crucially important to support high-affinity agonist binding of the receptor: Mg2+ and cholesterol, both acting as positive modulators.
Andrea, Schiffmann, Gerald, Gimpl
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Neurobiology of Stress, 2018 Stress-related substance use is a major challenge for treating substance use disorders. This selective review focuses on emerging pharmacotherapies with potential for reducing stress-potentiated seeking and consumption of nicotine, alcohol, marijuana ...
Mark K. Greenwald
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Natural Negative Allosteric Modulators of 5-HT₃ Receptors.
Molecules (Basel, Switzerland), 2019 Chemotherapy-induced nausea and vomiting (CINV) remain the most common and devastating side-effects associated with cancer chemotherapy. In recent decades, several lines of research emphasize the importance of 5-hydroxytryptamine3 (5-HT3; serotonin) receptors in the pathogenesis and treatment of CINV.
Lina T, Al Kury +3 more
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IUCrJ, 2018 The AMPA receptor GluA2 belongs to the family of ionotropic glutamate receptors, which are responsible for most of the fast excitatory neuronal signalling in the central nervous system. These receptors are important for memory and learning, but have also
Andreas Haahr Larsen +7 more
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A novel class of negative allosteric modulators of NMDA receptor function
Bioorganic & Medicinal Chemistry Letters, 2015 NMDA receptors mediate a slow Ca(2+)-permeable component of excitatory synaptic transmission, and are involved in numerous normal brain functions including learning and memory. NMDA receptor over-activation can lead to cell death and abnormal excitation in ischemia associated with stroke, traumatic brain injury, and epilepsy.
Brooke M. Katzman +6 more
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Nature CommunicationsAllosteric modulation is a central mechanism for metabolic regulation but has yet to be described for a gut microbiota-host interaction. Phenylacetylglutamine (PAGln), a gut microbiota-derived metabolite, has previously been clinically associated with ...
Prasenjit Prasad Saha +17 more
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