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Enzyme Kinetics and Drugs as Enzyme Inhibitors
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
As in other cases, allosteric drugs may be classified as covalent (see below) or noncovalent. To the latter belong the benzodiazepines, the non-benzodiazepine Z-drugs (zopiclone, zolpidem, etc.) or barbiturate drugs, targeting the ionotropic GABA receptor and acting as positive allosteric modulator molecules that increase the activity of the GABAA receptor protein in the central nervous system (e.g., Henschel et al., 2008). Cinacalcet is a positive G-protein-coupled receptor (GPCR) modulator that enhances Ca2+ activation of calcium-sensing receptor (Brown, 2010) and is employed to treat hyperparathyroidism; the cellular mechanisms for allosteric modulation of calcium-sensing receptors has been discussed by Cavanaugh et al. (2012). Maraviroc is a negative modulator of the GPCR chemokine receptor CCR5 and used for the treatment of HIV-type 1 (Conn et al., 2009, and literature cited therein). Metabotropic glutamate receptors (mGluRs, several different groups) involved in the modulation of synaptic transmission and neuronal excitability are members of the GPCR superfamily; mGluRs are drug targets of positive allosteric modulators for treating neurological and psychiatric disorders (Alzheimer’s, anxiety, schizophrenia, etc.) as reviewed by Niswender and Conn (2010), Wood et al. (2011), or Herman et al. (2012). A recent example are allosteric BCR-ABL tyrosine kinase fusion protein inhibitors in Philadelphia chromosome-positive acute lymphoblastic leukemia, developed to overcome resistance towards drugs like imatinib and others (Hantschel, 2012). For covalent allosteric inhibitors see the next section.
Structure elucidation capabilities on typical pharmaceutical drugs by new nuclear magnetic resonance technology: a 400 MHz high-temperature superconducting power-driven magnet NMR system
Published in Instrumentation Science & Technology, 2019
Maria Victoria Silva Elipe, Neil Donovan, Robert Krull, Donald Pooke, Kimberly L. Colson
The three compounds selected for this study contain fluorine as a trifluoromethyl group, which allowed us to obtain 19F NMR together with 1H and 13C NMR data to fully characterize their structures. Cinacalcet HCl, N-[(1R)-1-(naphthalen-1-yl)ethyl]-3-[3-(trifluoromethyl)phenyl]propan-1-amine – hydrogen chloride (1/1), (Figure 1) is the API of commercial oral formulated tablets that were approved in 2004 by the US Food and Drug Administration (FDA) as Sensipar and by the European Medicine Agency (EMEA) as Mimpara to treat patients with secondary hyperparathyroidism (sHPT) with chronic kidney disease (CKD) on dialysis.[4–8] In addition, cinacalcet HCl was approved for the treatment of primary hyperparathyroidism and parathyroid carcinoma in 2008 by EMEA and in 2011 by FDA.