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Cinacalcet therapy in a child with novel homozygous CASR p.Glu353Lys mutation causing familial hypocalciuric hypercalcemia type 1: case report and review of the literature
CONCLUSIONS: FHH can be seen in heterozygous as well as homozygous CASR gene mutations. Different clinical findings may occur in different individuals from the same family. Cinacalcet therapy can be used successfully in the treatment of individuals with FHH.PMID:37853976 | DOI:10.24953/turkjped.2022.1040 (Source: The Turkish Journal of Pediatrics)
Source: The Turkish Journal of Pediatrics - October 19, 2023 Category: Pediatrics Authors: Serkan Bilge Koca Source Type: research

Additive-Free Copper-Catalyzed Benzylic C(sp3) –H Carbamation: Simple Preparation of Primary Benzylic Amines
Synlett DOI: 10.1055/a-2170-2630 A simple and practical method for the synthesis of primary alkylamines by direct functionalization of hydrocarbons is described. The N-Boc-protected alkylamines are readily prepared from tert-butyl (trimethylsilyl)carbamate and N-fluorobenzenesulfonimide in the presence of a Cu(I) catalyst at low catalyst loadings. Advantageously, this process proceeds free of any additive such as auxiliary bases/acids, requires only one equivalent of the substrate, and does not require ligand synthesis. This operationally simple C–H carbamation method shows high site selectivity and good functional-group...
Source: Synlett - October 12, 2023 Category: Chemistry Authors: Schmidt, William Bakhoda, Abolghasem Gus Tags: letter Source Type: research

Effect of Paricalcitol Combined with Cinacalcet on Calcium and Phosphorus Metabolism in Patients Receiving Maintenance Hemodialysis
This study was designed to compare the beneficial effects of paricalcitol combined with or without cinacalcet on calcium and phosphorus metabolism in patients undergoing maintenance hemodialysis (MHD). A total of 140 patients who received MHD in our hospital from March 2021 to March 2022 were randomly divided into a control group (intravenous paricalcitol, n = 70) and a test group (intravenous paricalcitol combined with oral cinacalcet, n = 70). Clinical baseline data and relevant laboratory parameters before treatment were compared. Additionally, calcium, phosphorus, intact parathyroid hormone in serum were measured and c...
Source: Clinical Pharmacology in Drug Development - October 10, 2023 Category: Drugs & Pharmacology Authors: Feng ‐yun Zheng, Ya‐yin Tan, Jia‐jun Zhou Tags: Original Article Source Type: research

Calcium-sensing receptor activator cinacalcet for treatment of cyclic nucleotide-mediated secretory diarrheas
CONCLUSIONS: Our findings suggest that CaSR activator cinacalcet has antidiarrheal efficacy in distinct human cell, organoid and mouse models of secretory diarrhea. Considering its excellent clinical safety profile, cinacalcet can be repurposed as a treatment for secretory diarrheas including cholera.PMID:37678755 | DOI:10.1016/j.trsl.2023.09.001 (Source: Translational Research : the journal of laboratory and clinical medicine)
Source: Translational Research : the journal of laboratory and clinical medicine - September 7, 2023 Category: Laboratory Medicine Authors: Tifany Chu Pattareeya Yottasan Livia de Souza Goncalves Apurva A Oak Ruxian Lin Ming Tse Mark Donowitz Onur Cil Source Type: research

Calcium-sensing receptor activator cinacalcet for treatment of cyclic nucleotide-mediated secretory diarrheas
CONCLUSIONS: Our findings suggest that CaSR activator cinacalcet has antidiarrheal efficacy in distinct human cell, organoid and mouse models of secretory diarrhea. Considering its excellent clinical safety profile, cinacalcet can be repurposed as a treatment for secretory diarrheas including cholera.PMID:37678755 | DOI:10.1016/j.trsl.2023.09.001 (Source: Cell Research)
Source: Cell Research - September 7, 2023 Category: Cytology Authors: Tifany Chu Pattareeya Yottasan Livia de Souza Goncalves Apurva A Oak Ruxian Lin Ming Tse Mark Donowitz Onur Cil Source Type: research

Calcium-sensing receptor activator cinacalcet for treatment of cyclic nucleotide-mediated secretory diarrheas
: Cyclic nucleotide elevation in intestinal epithelial cells is the key pathology causing intestinal fluid loss in secretory diarrheas such as cholera. Current secretory diarrhea treatment is primarily supportive, and oral rehydration solution is the mainstay of cholera treatment. There is an unmet need for safe, simple and effective diarrhea treatments. By promoting cAMP hydrolysis, extracellular calcium-sensing receptor (CaSR) is a regulator of intestinal fluid transport. (Source: Translational Research)
Source: Translational Research - September 5, 2023 Category: Research Authors: Tifany Chu, Pattareeya Yottasan, Livia de Souza Goncalves, Apurva A. Oak, Ruxian Lin, Ming Tse, Mark Donowitz, Onur Cil Source Type: research

Reduction of esters to alcohols and iodides using aminodiborane ( μ-NH 2 B 2 H 5 ): scope and mechanistic investigations
Chem Commun (Camb). 2023 Aug 30. doi: 10.1039/d3cc03100d. Online ahead of print.ABSTRACTHerein, we report an efficient methodology for the reduction of esters, carbonates, and anhydrides to alcohols using in situ generated aminodiborane from iodine and ammonia borane. This methodology also finds use for the transformation of esters to iodides by varying the stoichiometry of reagents. The protocol has broad substrate scope for transformation of esters to alcohols and iodides with excellent yields. The method is also useful for synthesizing pharmaceutically and industrially important compounds such as a Cinacalcet precursor,...
Source: Chemical Communications - August 30, 2023 Category: Chemistry Authors: Abhishek Nair Vikas Tiwari Sambhav Rath Parul Saini Ashutosh Verma Anil J Elias Source Type: research

Cinacalcet reverses short QT interval in Familial Hypocalciuric Hypercalcemia type 1
CONCLUSION: Our results indicate that FHH-1 patients should be assessed for a short QT interval, and a cinacalcet test used to select patients who are likely to benefit from this treatment.PMID:37602721 | DOI:10.1210/clinem/dgad494 (Source: The Journal of Clinical Endocrinology and Metabolism)
Source: The Journal of Clinical Endocrinology and Metabolism - August 21, 2023 Category: Endocrinology Authors: Thomas Cuny Pauline Romanet Michelle Goldsworthy Carole Gu érin Marie Wilkin Philippe Roche Fr édéric Sebag Lynn E van Summeren Mark Stevenson Sarah A Howles Jean-Claude Deharo Rajesh V Thakker David Ta ïeb Source Type: research

Molecules, Vol. 28, Pages 6042: Improved Process for the Synthesis of 3-(3-Trifluoromethylphenyl)propanal for More Sustainable Production of Cinacalcet HCl
Piccolo Cinacalcet (I), sold as hydrochloride salt, is a calcimimetic drug which has been approved for the treatment of secondary hyperparathyroidism in patients with chronic renal disease and for the treatment of hypercalcemia in patients with parathyroid carcinoma. Here, an improved method for the synthesis of 3-(3-trifluoromethylphenyl)propanal (II), a key intermediate for the preparation of I, is described. The protocol required a Mizoroki&ndash;Heck cross-coupling reaction between 1-bromo-3-(trifluoromethyl)benzene and acroleine diethyl acetal, catalyzed by Pd(OAc)2 in the presence of nBu4NOAc (tetrabutyl...
Source: Molecules - August 13, 2023 Category: Chemistry Authors: Vikas Damu Rathod Stefano Paganelli Marijan Ko čevar Marko Krivec Oreste Piccolo Tags: Article Source Type: research

Pharmacological profile of upacicalcet, a novel positive allosteric modulator of calcium-sensing receptor, in vitro and in vivo
Eur J Pharmacol. 2023 Aug 2:175936. doi: 10.1016/j.ejphar.2023.175936. Online ahead of print.ABSTRACTUpacicalcet (formerly SK-1403/AJT240) is a novel non-peptide calcimimetic agent that acts as a calcium-sensing receptor (CaSR) agonist for the treatment of secondary hyperparathyroidism (SHPT) in chronic kidney disease (CKD). We compared upacicalcet with other calcimimetics (etelcalcetide or cinacalcet) and examined its in vitro and in vivo characteristics in terms of its human CaSR agonistic activity, its efficacy in normal and CKD rats after a single administration, and its effect on gastric emptying in rats. Upacicalcet ...
Source: European Journal of Pharmacology - August 4, 2023 Category: Drugs & Pharmacology Authors: Moritaka Goto Go Nishimura Hirofumi Sato Yu Yamaguchi Nobutaka Morimoto Hiroyuki Hashimoto Naoki Takahashi Source Type: research