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CGRP antagonists

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https://www.readbyqxmd.com/read/28627595/elevated-expression-of-transient-receptor-potential-vanilloid-type%C3%A2-1-in-dorsal-root-ganglia-of-rats-with-endometriosis
#1
Yu-Ling Lian, Ming-Jun Cheng, Xian-Xia Zhang, Li Wang
Pain is the most pronounced complaint of women with endometriosis, however the underlying mechanism is still poorly understood. In the present study, the authors evaluate the effect of transient receptor potential vanilloid type 1 (TRPV1) of dorsal root ganglia (DRG) on endometriosis-associated pain. A total of 36 SD rats were randomly divided into a sham group (n=9) and a Model group (n=27), accepted auto‑transplanted pieces of fat or uterus to the pelvic cavity. At 4 weeks, the Model group was randomly subdivided into the following groups: ENDO group (no treatment, n=9), BCTC group (Model + BCTC, an antagonist of TRPV1, n=9), Vehicle group (Model + cyclodextrin, the vehicle of BCTC, n=9)...
June 15, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28604219/potentiation-of-nmda-receptor-mediated-synaptic-transmission-at-the-parabrachial-central-amygdala-synapses-by-cgrp-in-mice
#2
Yuya Okutsu, Yukari Takahashi, Masashi Nagase, Kei Shinohara, Ryo Ikeda, Fusao Kato
The capsular part of the central amygdala (CeC) is called the "nociceptive amygdala," as it receives nociceptive information from various pathways, including monosynaptic input from the lateral part of the parabrachial nucleus (LPB), a major target of ascending neurons in the spinal and medullary dorsal horn. LPB-CeC synaptic transmission is mediated by glutamate but the fibers from the LPB also contain calcitonin gene-related peptide (CGRP) and the CeC is rich in CGRP-binding sites. CGRP might be released in response to strong nociception and activate these CGRP receptors...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28560541/differential-inhibitory-response-to-telcagepant-on-%C3%AE-cgrp-induced-vasorelaxation-and-intracellular-ca-2-levels-in-the-perfused-and-non-perfused-isolated-rat-middle-cerebral-artery
#3
André Erdling, Majid Sheykhzade, Lars Edvinsson
BACKGROUND: Calcitonin gene-related peptide (CGRP) is one of the most potent endogenous vasodilators identified to date. The present study elucidates the differential interaction of CGRP, its receptor and the effect of the CGRP-receptor antagonist telcagepant on intracellular Ca(2+) -levels and tension in rat middle cerebral arteries (MCA) by pressurized arteriography, FURA-2/wire myography and immunohistochemistry. METHODS: A pressurized arteriograph system was used to evaluate changes in MCA tension when subjected to CGRP and/or telcagepant...
December 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28540451/exogenous-cgrp-upregulates-profibrogenic-growth-factors-through-pkc-jnk-signaling-pathway-in-kidney-proximal-tubular-cells
#4
Sang Pil Yoon, Jinu Kim
Kidney denervation prevents the development of tubulointerstitial fibrosis, but the neuropeptide calcitonin gene-related peptide (CGRP) in the denervated kidneys restores the fibrotic feature through the upregulation of profibrogenic growth factors. CGRP is involved in aggravation of inflammation by increasing the number of circulating cells and chemotactic factors. However, it is not clear how CGRP contributes to the upregulation of profibrogenic factors during fibrogenesis. In both human and pig kidney proximal tubular cell lines, administration of 1 nM CGRP significantly increased the levels of transforming growth factor-β1 (TGF-β1) production and connective tissue growth factor (CTGF) expression at 6 and 24 h after the administration...
May 24, 2017: Cell Biology and Toxicology
https://www.readbyqxmd.com/read/28527051/new-treatments-for-headache
#5
Kasra Maasumi, Stewart J Tepper, Alan M Rapoport
Headache disorders are common worldwide and often disabling. Until recently, treatments were borrowed from other branches of neurology and medicine. Monoclonal antibodies targeting calcitonin gene-related peptide (CGRP) ligand and receptor, small molecule CGRP receptor antagonist gepants, serotonin1F agonists, new devices to deliver currently available drugs, and neuromodulation devices have recently been in the forefront of headache treatments that are rather specific for various headache disorders. These novel therapies are changing the field of headache medicine...
May 2017: Neurological Sciences
https://www.readbyqxmd.com/read/28497257/-therapy-of-migranes
#6
D Holle-Lee, S Nägel, C Gaul
In migraine attack treatment analgesics such as nonsteroidal anti-inflammatory drugs and triptans can be utilized. The efficacy of acute attack treatment is relevant to prevent migraine chronification. For prophylactic treatment β‑blockers, tricyclic antidepressants, flunarizine, antiepileptics and onabotulinumtoxin A are available. There is evidence that some other substances (e. g. sartans) are also efficacious in this regard. Furthermore, nondrug approaches are essential in migraine therapy. Early education and prophylactic treatment of patients at risk may prevent from medication overuse headache...
May 11, 2017: Der Nervenarzt
https://www.readbyqxmd.com/read/28496430/cholinergic-nociceptive-mechanisms-in-rat-meninges-and-trigeminal-ganglia-potential-implications-for-migraine-pain
#7
Irina Shelukhina, Nikita Mikhailov, Polina Abushik, Leniz Nurullin, Evgeny E Nikolsky, Rashid Giniatullin
BACKGROUND: Parasympathetic innervation of meninges and ability of carbachol, acetylcholine (ACh) receptor (AChR) agonist, to induce headaches suggests contribution of cholinergic mechanisms to primary headaches. However, neurochemical mechanisms of cholinergic regulation of peripheral nociception in meninges, origin place for headache, are almost unknown. METHODS: Using electrophysiology, calcium imaging, immunohistochemistry, and staining of meningeal mast cells, we studied effects of cholinergic agents on peripheral nociception in rat hemiskulls and isolated trigeminal neurons...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/28485848/the-trigeminovascular-pathway-role-of-cgrp-and-cgrp-receptors-in-migraine
#8
REVIEW
Lars Edvinsson
The trigeminal ganglion plays a key role in primary headache pathophysiology. Calcitonin gene-related peptide (CGRP) and CGRP receptors are expressed in trigeminal neurons that form C-fibers and A-fibers, respectively. In acute migraine and cluster headache attacks, there is release of CGRP into the cranial venous outflow. In addition, intravenous CGRP can induce migraine-like symptoms in migraine patients. These findings led to the development of anti-migraine therapies that inhibit CGRP action. Currently, CGRP receptor antagonists, the gepants, and monoclonal antibodies towards CGRP and the CGRP receptor are all showing positive relief of acute and chronic migraine in clinical trials...
May 2017: Headache
https://www.readbyqxmd.com/read/28470555/cgrp-8-37-enhances-lipopolysaccharide-induced-acute-lung-injury-and-regulating-aquaporin-1-and-5-expressions-in-rats
#9
Fu Hong-Min, Huangfu Chun-Rong, Zheng Rui, Su Li-Na, Wang Ya-Jun, Li Li
Calcitonin gene-related peptide (CGRP) has been shown to play important roles in biological functions. However, there is very little evidence on the value of CGRP in lipopolysaccharide (LPS)-induced acute lung injury/acute respiratory distress syndrome (ALI/ARDS). Therefore, this study aimed to investigate the role of CGRP in LPS-induced ALI in rats. In the experiment, Sprague-Dawley (SD) rats were randomized into control, an antagonist of α-calcitonin gene-related peptide receptor (CGRP8-37), LPS groups, and CGRP8-37 + LPS groups...
May 4, 2017: Journal of Physiology and Biochemistry
https://www.readbyqxmd.com/read/28446517/a-novel-%C3%AE-calcitonin-gene-related-peptide-analogue-protects-against-end-organ-damage-in-experimental-hypertension-cardiac-hypertrophy-and-heart-failure
#10
Aisah A Aubdool, Pratish Thakore, Fulye Argunhan, Sarah-Jane Smillie, Moritz Schnelle, Salil Srivastava, Khadija M Alawi, Elena Wilde, Jennifer Mitchell, Keith Farrell-Dillon, Daniel A Richards, Giuseppe Maltese, Richard C Siow, Manasi Nandi, James E Clark, Ajay M Shah, Anette Sams, Susan D Brain
Background -Research into the therapeutic potential of α-calcitonin gene-related peptide (α-CGRP) has been limited due to its peptide nature and short half-life. Here, we evaluate whether a novel potent and long lasting (t½ ≥ 7h) acylated α-CGRP analogue (αAnalogue) could alleviate and reverse cardiovascular disease in two distinct murine models of hypertension and heart failure in vivoMethods -The ability of the αAnalogue to act selectively via the CGRP pathway was shown in skin using a CGRP receptor antagonist...
April 26, 2017: Circulation
https://www.readbyqxmd.com/read/28413467/calcitonin-gene-related-peptide-protects-type-ii-alveolar-epithelial-cells-from-hyperoxia-induced-dna-damage-and-cell-death
#11
Hongmin Fu, Tiesong Zhang, Rongwei Huang, Zhen Yang, Chunming Liu, Ming Li, Fang Fang, Feng Xu
Hyperoxia therapy for acute lung injury (ALI) may unexpectedly lead to reactive oxygen species (ROS) production and cause additional ALI. Calcitonin gene-related peptide (CGRP) is a 37 amino acid neuropeptide that regulates inflammasome activation. However, the role of CGRP in DNA damage during hyperoxia is unclear. Therefore, the aim of the present study was to investigate the effects of CGRP on DNA damage and the cell death of alveolar epithelial type II cells (AEC II) exposed to 60% oxygen. AEC II were isolated from 19-20 gestational day fetal rat lungs and were exposed to air or to 60% oxygen during treatment with CGRP or the specific CGRP receptor antagonist CGRP8-37...
April 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28376659/kappa-opioid-receptor-antagonists-a-possible-new-class-of-therapeutics-for-migraine-prevention
#12
Jennifer Y Xie, Milena De Felice, Caroline M Kopruszinski, Nathan Eyde, Justin LaVigne, Bethany Remeniuk, Pablo Hernandez, Xu Yue, Naomi Goshima, Michael Ossipov, Tamara King, John M Streicher, Edita Navratilova, David Dodick, Hugh Rosen, Ed Roberts, Frank Porreca
Background Stress is the most commonly reported migraine trigger. Dynorphin, an endogenous opioid peptide acting preferentially at kappa opioid receptors (KORs), is a key mediator of stress responses. The aim of this study was to use an injury-free rat model of functional cephalic pain with features of migraine and medication overuse headache (MOH) to test the possible preventive benefit of KOR blockade on stress-induced cephalic pain. Methods Following sumatriptan priming to model MOH, rats were hyper-responsive to environmental stress, demonstrating delayed cephalic and extracephalic allodynia and increased levels of CGRP in the jugular blood, consistent with commonly observed clinical outcomes during migraine...
January 1, 2017: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/28369749/olcegepant-blocks-neurogenic-and-non-neurogenic-cgrpergic-vasodepressor-responses-and-facilitates-noradrenergic-vasopressor-responses-in-pithed-rats
#13
V H Avilés-Rosas, E Rivera-Mancilla, B A Marichal-Cancino, G Manrique-Maldonado, A H Altamirano-Espinoza, A MaassenVanDenBrink, C M Villalón
BACKGROUND AND PURPOSE: Olcegepant (BIBN4096BS) is a selective non-peptide CGRP receptor antagonist with acute antimigraine properties. Since systemic vascular tone is modulated by perivascular (primary sensory CGRPergic and sympathetic) nerves, this randomized study investigated in pithed rats the effect of acute i.v. treatment with olcegepant on the neurogenic and non-neurogenic: (i) CGRPergic vasodepressor responses; and (ii) noradrenergic vasopressor responses. The pithed rat is an experimental model predictive of systemic (cardio) vascular side effects...
March 29, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28364596/cardioprotective-effects-of-calcitonin-gene-related-peptide-in-isolated-rat-heart-and-in-h9c2-cells-via-redox-signaling
#14
Francesca Tullio, Claudia Penna, Karine Cabiale, Saveria Femminò, Marco Galloni, Pasquale Pagliaro
The calcitonin-gene-related-peptide (CGRP) release is coupled to the signaling of Angeli's salt in determining vasodilator effects. However, it is unknown whether CGRP is involved in Angeli's salt cardioprotective effects and which are the mechanisms of protection. We aimed to determine whether CGRP is involved in myocardial protection induced by Angeli's salt. We also analyzed the intracellular signaling pathway activated by CGRP. Isolated rat hearts were pre-treated with Angeli's salt or Angeli's salt plus CGRP8-37, a specific CGRP-receptor antagonist, and subjected to ischemia (30-min) and reperfusion (120-min)...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28355142/effects-of-adrenomedullin-and-glucagon-like-peptide-on-distal-flap-necrosis-and-vascularity-the-role-of-receptor-systems-and-nitric-oxide
#15
Betul Cam, Deniz Bagdas, M Ozgur Ozyigit, Engin Sagdilek, Naciye Isbil Buyukcoskun, Kasım Ozluk
OBJECTIVE: Flap necrosis in the distal area due to the deficiency of blood circulation is a major complication in flap treatment. In many previous studies, some natural substances such as chlorogenic acid, adrenomedullin (ADM), and glucagon-like peptide-1 (GLP-1) have been used to improve flap viability via their vasodilator, angiogenic, and antioxidant effects. The aim of this study is to clarify the mechanism through the use of selective antagonists for calcitonin gene-related peptide (CGRP) receptors and GLP-1 receptors such as CGRP-(8-37), exendin-(9-39), respectively, in the flap healing effects of ADM and GLP-1...
March 24, 2017: Wounds: a Compendium of Clinical Research and Practice
https://www.readbyqxmd.com/read/28321564/an-update-on-migraine-current-understanding-and-future-directions
#16
Francesca Puledda, Roberta Messina, Peter J Goadsby
Migraine is a common brain disorder with high disability rates which involves a series of abnormal neuronal networks, interacting at different levels of the central and peripheral nervous system. An increase in the interest around migraine pathophysiology has allowed researchers to unravel certain neurophysiological mechanisms and neurotransmitter involvement culminating in the recent development of novel therapies, which might substantially change the clinical approach to migraine patients. The present review will highlight the current aspects of migraine pathophysiology, covering an understanding of the complex workings of the migraine state and the brain regions responsible for them...
March 20, 2017: Journal of Neurology
https://www.readbyqxmd.com/read/28317098/cgrp-receptor-activity-in-mice-with-global-expression-of-human-receptor-activity-modifying-protein-1
#17
Keegan J Bohn, Baolin Li, Xiaofang Huang, Bianca N Mason, Anne-Sophie Wattiez, Adisa Kuburas, Christopher S Walker, Peiyi Yang, Jianliang Yu, Beverly A Heinz, Kirk W Johnson, Andrew F Russo
BACKGROUND AND PURPOSE: CGRP is a potent vasodilator and nociceptive neuropeptide linked to migraine. CGRP receptors are heterodimers of receptor activity modifying protein 1 (RAMP1) and either calcitonin receptor-like receptor (CLR; forms canonical CGRP receptor) or calcitonin receptor (CT receptor; forms AMY1 receptor). The goal of this study was to test whether transgenic mice globally expressing human RAMP1 have increased CGRP receptor activity and whether the receptors are sensitive to human selective antagonist telcagepant...
June 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28306261/asymmetric-synthesis-of-the-major-metabolite-of-a-calcitonin-gene-related-peptide-receptor-antagonist-and-mechanism-of-epoxide-hydrogenolysis
#18
Guanglin Luo, Ling Chen, Charles M Conway, Walter Kostich, Benjamin M Johnson, Alicia Ng, John E Macor, Gene M Dubowchik
An asymmetric synthesis of the major metabolite of the calcitonin gene-related peptide recepotor antagonist BMS-846372 is presented. The variously substituted cyclohepta[b]pyridine ring system represents an underexplored ring system and showed some unexpected chemistry. Reactivities of epoxide and ketone functional groups on the cycloheptane ring were extensively controlled by a remote bulky TIPS group. The rate difference of the hydrogenolysis between two diastereomeric epoxide intermediates shed some light on the mechanism of epoxide hydrogenolysis, and further, deuterium labeling studies revealed more mechanistic details on this well-known chemical transformation for the first time...
March 28, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28254863/bone-pain-induced-by-multiple-myeloma-is-reduced-by-targeting-v-atpase-and-asic3
#19
Masahiro Hiasa, Tatsuo Okui, Yohance M Allette, Matthew S Ripsch, Ge-Hong Sun-Wada, Hiroki Wakabayashi, G David Roodman, Fletcher A White, Toshiyuki Yoneda
Multiple myeloma patients experience severe bone pain (MMBP) that is undertreated and poorly understood. In this study, we studied MMBP in an intratibial mouse xenograft model that employs JJN3 human multiple myeloma cells. In this model, mice develop MMBP associated in bone with increased sprouting of calcitonin gene-related peptide-positive (CGRP(+)) sensory nerves and in dorsal root ganglia (DRG) with upregulation of phosphorylated ERK1/2 (pERK1/2) and pCREB, two molecular indicators of neuron excitation...
March 15, 2017: Cancer Research
https://www.readbyqxmd.com/read/28205139/the-potentiating-effect-of-calcitonin-gene-related-peptide-on-transient-receptor-potential-vanilloid-1-activity-and-the-electrophysiological-responses-of-rat-trigeminal-neurons-to-nociceptive-stimuli
#20
Duangthip Chatchaisak, Mark Connor, Anan Srikiatkhachorn, Banthit Chetsawang
Growing evidence suggests that calcitonin gene-related peptide (CGRP) participates in trigeminal nociceptive responses. However, the role of CGRP in sensitization or desensitization of nociceptive transduction remains poorly understood. In this study, we sought to further investigate the CGRP-induced up-regulation of transient receptor potential vanilloid-1 (TRPV1) and the responses of trigeminal neurons to nociceptive stimuli. Rat trigeminal ganglion (TG) organ cultures and isolated trigeminal neurons were incubated with CGRP...
February 15, 2017: Journal of Physiological Sciences: JPS
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