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https://www.readbyqxmd.com/read/29435045/the-protective-effects-of-rutaecarpine-on-acute-pancreatitis
#1
Lu Yan, Qing-Fu Li, Yan-Ting Rong, Yong-Heng Chen, Zhao-Hong Huang, Zhi-Zhi Wang, Jie Peng
Acute pancreatitis (AP) is the acute inflammation of the pancreas. The morbidity of AP has increased in recent years. Certain patients eventually develop severe AP (SAP), which rapidly progresses to multiple organ dysfunction; the incidence of this occurring in patients with AP is 20-30%. To date, no specific drugs or methods exist to treat this disease. Rutaecarpine relaxes vascular smooth muscle by stimulating calcitonin gene-related peptide (CGRP) release via activation of vanilloid receptor subtype 1 (VR1)...
March 2018: Oncology Letters
https://www.readbyqxmd.com/read/29430561/the-cgrp-receptor-antagonist-bibn4096-inhibits-prolonged-meningeal-afferent-activation-evoked-by-brief-local-k-stimulation-but-not-cortical-spreading-depression-induced-afferent-sensitization
#2
Jun Zhao, Dan Levy
Introduction: Cortical spreading depression (CSD) is believed to promote migraine headache by enhancing the activity and mechanosensitivity of trigeminal intracranial meningeal afferents. One putative mechanism underlying this afferent response involves an acute excitation of meningeal afferents by cortical efflux of K + and the ensuing antidromic release of proinflammatory sensory neuropeptides, such as calcitonin gene-related peptide (CGRP). Objectives: We sought to investigate whether (1) a brief meningeal K + stimulus leads to CGRP-dependent enhancement of meningeal afferent responses and (2) CSD-induced meningeal afferent activation and sensitization involve CGRP receptor signaling...
January 2018: Pain Reports (Baltimore, Md.)
https://www.readbyqxmd.com/read/29416550/the-wnt7b-%C3%AE-catenin-signaling-pathway-is-involved-in-the-protective-action-of-calcitonin-gene-related-peptide-on-hyperoxia-induced-lung-injury-in-premature-rats
#3
Shaohua Wang, Hongxing Dang, Feng Xu, Jian Deng, Xuemei Zheng
Background: Calcitonin gene-related peptide (CGRP) can protect against hyperoxia-induced lung injury, making the upregulation of CGRP a potential therapeutic approach for this type of injury. However, the effects of CGRP on the Wnt7b/β-catenin signaling pathway are unclear. In this study, we investigated the roles of CGRP and the Wnt7b/β-catenin signaling pathway in hyperoxia-induced lung injury. Methods: Premature Sprague Dawley (SD) rats were exposed to 21, 40, 60 and 95% oxygen for 3, 7 and 14 days...
2018: Cellular & Molecular Biology Letters
https://www.readbyqxmd.com/read/29396376/calcitonin-gene-related-peptide-is-a-potent-inducer-of-oedema-in-rat-orofacial-tissue
#4
Bárbara F G de Queiroz, Marcella P A de Almeida, Y S Bakhle, Janetti N Francischi
BACKGROUND AND AIMS: This study aimed to assess the potential of calcitonin-gene related peptide (CGRP), a neuropeptide released from sensory nerves, to induce oedema in orofacial tissue. EXPERIMENTAL APPROACH: Wistar rats (150-200 g) anesthetized with isoflurane were injected intraorally with CGRP (100 μl; 8-33 pmol) in the right side of the mouth. The contralateral side was injected with the same volume of physiological saline. Increased cheek thickness (in mm), as a measure of oedema formation, was assayed bilaterally with a digital caliper before (T = 0) and up to 24 h following injection of CGRP...
January 30, 2018: Neuropeptides
https://www.readbyqxmd.com/read/29393417/involvement-of-trpv1-in-the-expression-and-release-of-calcitonin-gene-related-peptide-induced-by-rutaecarpine
#5
Yongmei Yang, Qingquan Chen, Sujie Jia, Limei He, Aiping Wang, Dai Li, Yuanjian Li, Xiaohui Li
The traditional Chinese herb Wu-Chu-Yu has been used to treat hypertension for hundreds of years. A previous study indicated that rutaecarpine was the effective component of Wu‑Chu‑Yu, which lowered blood pressure by elevating the expression level of calcitonin gene‑related peptide (CGRP). The present study was performed to investigate the role of transient receptor potential cation channel subfamily V member 1 (TRPV1) in CGRP expression and release induced by rutaecarpine. Dorsal root ganglia (DRG) obtained from Sprague‑Dawley rats were cultured to analyze the mRNA expression and release of CGRP...
January 25, 2018: Molecular Medicine Reports
https://www.readbyqxmd.com/read/29382888/a-unique-inbred-rat-strain-with-sustained-cephalic-hypersensitivity-as-a-model-of-chronic-migraine-like-pain
#6
Gordon Munro, Steffen Petersen, Inger Jansen-Olesen, Jes Olesen
Animal models of migraine-like pain enabling ongoing study of behaviour typically involve the systemic administration of chemical vasodilators or dural administration of inflammatory algogens. However, neither method mediates prolonged effects on behavior indicative of enduring pathophysiological changes occurring within dural or trigeminal pain circuits. We generated successive generations of a unique inbred rat strain, spontaneous trigeminal allodynia (STA) rats, previously reported to exhibit an episodic migraine-like behavioural phenotype...
January 30, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29363552/probing-the-mechanism-of-receptor-activity-modifying-protein-modulation-of-gpcr-ligand-selectivity-through-rational-design-of-potent-adrenomedullin-and-calcitonin-gene-related-peptide-antagonists
#7
Jason M Booe, Margaret L Warner, Amanda M Roehrkasse, Debbie L Hay, Augen A Pioszak
Binding of the vasodilator peptides adrenomedullin (AM) and calcitonin gene-related peptide (CGRP) to the class B GPCR calcitonin receptor-like receptor (CLR) is modulated by receptor activity-modifying proteins (RAMP). RAMP1 favors CGRP, whereas RAMP2 and RAMP3 favor AM. Crystal structures of peptide-bound RAMP1/2-CLR extracellular domain (ECD) heterodimers suggested RAMPs alter ligand preference through direct peptide contacts and allosteric modulation of CLR. Here, we probed this dual mechanism through rational structure-guided design of AM and CGRP antagonist variants...
January 23, 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/29353067/antinociception-of-the-spirocyclopiperazinium-salt-compound-lxm-15-via-activating-%C3%AE-7-nachr-and-m4-machr-and-inhibiting-camkii%C3%AE-camp-creb-cgrp-signalling-pathway-in-mice
#8
Hua Yang, Qi Sun, Yingying Liang, Yimin Jiang, Runtao Li, Jia Ye
The aim of this study was to investigate the analgesic effect of the spirocyclopiperazinium salt compound LXM-15 by intragastric administration in thermal and chemical pain models and further to elucidate the possible molecular mechanisms. The results showed that LXM-15 exerted significant antinociception in hot-plate test, formalin test and acetic acid writhing test. Western blot analysis showed that LXM-15 significantly reduced the upregulation of phosphorylation of calcium/calmodulin -dependent protein kinaseⅡα (CaMKIIα) and cAMP response element-binding protein (CREB), and further decreased the elevation of calcitonin gene related peptide (CGRP) in the dorsal root ganglion (DRG) and spinal cord in mice...
January 15, 2018: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/29350125/current-management-migraine-headache
#9
Stephen D Silberstein
Migraine varies in its frequency, severity, and impact; treatment should consider these variations and the patient's needs and goals. Migraine pharmacologic treatment may be acute (abortive) or preventive (prophylactic), and patients often require both. New medication devices are available or in development, including an intracutaneous, microneedle system of zolmitriptan and sumatriptan, and breath-powered powder sumatriptan intranasal treatment. Lasmiditan, a 5-HT1F receptor agonist, is in development for acute treatment, as are small molecule calcitonin gene-related peptide (CGRP) receptor antagonists (Gepants) for acute and preventive treatment...
December 2017: CNS Spectrums
https://www.readbyqxmd.com/read/29335794/effect-of-a-calcitonin-gene-related-peptide-binding-l-rna-aptamer-on-neuronal-activity-in-the-rat-spinal-trigeminal-nucleus
#10
Michael J M Fischer, Jakob Schmidt, Stanislav Koulchitsky, Sven Klussmann, Axel Vater, Karl Messlinger
BACKGROUND: Calcitonin gene-related peptide (CGRP) plays a major role in the pathogenesis of migraine and other primary headaches. Spinal trigeminal neurons integrate nociceptive afferent input from trigeminal tissues including intracranial afferents, and their activity is thought to reflect facial pain and headache in man. CGRP receptor inhibitors and anti-CGRP antibodies have been demonstrated to be therapeutically effective in migraine. In parallel, CGRP receptor inhibition has been shown to lower spinal trigeminal neuron activity in animal models of meningeal nociception...
January 15, 2018: Journal of Headache and Pain
https://www.readbyqxmd.com/read/29288742/the-research-of-the-possible-mechanism-and-the-treatment-for-capsaicin-induced-cough
#11
Li Zhang, Tieying Sun, Longteng Liu, Lifang Wang
Unexplained chronic cough (UCC) affects millions of patients worldwide. New therapeutic approaches to this condition are urgently needed, since current treatment options provide only symptomatic relief. Cough reflex hypersensitivity has been shown to play an important role in the pathogenesis of UCC. The transient receptor potential vanilloid type 1 (TRPV1) is present on peripheral terminals of airway sensory nerves and modulation of its activity represents a potential target for the pharmacological treatment of UCC...
December 27, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29276263/calcitonin-gene-related-peptide-receptor-antagonists-for-migraine-prophylaxis
#12
Scot Walker
Migraine is a common disorder affecting 12% of the U.S. POPULATION: Prophylaxis is recommended for patients who experience frequent migraines. Because current drugs used for prophylaxis are not 100% effective and cause adverse effects that affect compliance, new strategies have been studied to prevent headaches. One new pharmacologic strategy is to use an inhibitor of the calcitonin gene-related peptide (CGRP). As a class, the CGRP receptor inhibitors have reduced monthly migraine days and are well tolerated...
June 2017: Hospital Pharmacy
https://www.readbyqxmd.com/read/29226741/side-effects-associated-with-current-and-prospective-antimigraine-pharmacotherapies
#13
REVIEW
Abimael González-Hernández, Bruno A Marichal-Cancino, Antoinette MaassenVanDenBrink, Carlos M Villalón
Migraine is a neurovascular disorder. Current acute specific antimigraine pharmacotherapies target trigeminovascular 5-HT1B/1D, 5-HT1F and CGRP receptors but, unfortunately, they induce some cardiovascular and central side effects that lead to poor treatment adherence/compliance. Therefore, new antimigraine drugs are being explored. Areas covered: This review considers the adverse (or potential) side effects produced by current and prospective antimigraine drugs, including medication overuse headache (MOH) produced by ergots and triptans, the side effects observed in clinical trials for the new gepants and CGRP antibodies, and a section discussing the potential effects resulting from disruption of the cardiovascular CGRPergic neurotransmission...
January 2018: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29136283/population-pk-analyses-of-ubrogepant-mk-1602-a-cgrp-receptor-antagonist-enriching-in-clinic-plasma-pk-sampling-with-outpatient-dried-blood-spot-sampling
#14
Chi-Chung Li, Marissa Dockendorf, Ken Kowalski, Bei Yang, Yang Xu, Iris Xie, Huub Jan Kleijn, Rolien Bosch, Christopher Jones, Bob Thornton, Eugene E Marcantonio, Tiffini Voss, Kevin P Bateman, Prajakti A Kothare
Merck & Co., Inc. (Kenilworth, New Jersey) has recently published an integrated strategy for implementation of dried blood spots (DBS) in late-stage trials for population pharmacokinetic (PK) modeling. We applied this strategy for another late-stage clinical program: ubrogepant (MK-1602), a novel oral calcitonin gene-related peptide receptor antagonist for acute treatment of migraine. At the time of implementation, ubrogepant was entering phase 2 development. DBS was implemented to acquire PK information proximal to an acute migraine event to enable exposure-response modeling...
November 14, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29134730/role-of-central-versus-peripheral-opioid-system-in-antinociceptive-and-anti-inflammatory-effect-of-botulinum-toxin-type-a-in-trigeminal-region
#15
V Drinovac Vlah, B Filipović, L Bach-Rojecky, Z Lacković
BACKGROUND: Although botulinum toxin type A (BT-A) is approved for chronic migraine treatment, its site and mechanism of action are still elusive. Recently our group discovered that suppression of CGRP release from dural nerve endings might account for antimigraine action of pericranially injected BT-A. We demonstrated that central antinociceptive effect of BT-A in sciatic region involves endogenous opioid system as well. Here we investigated possible interaction of BT-A with endogenous opioid system within the trigeminal region...
November 13, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/29116598/cgrp-monoclonal-antibodies-for-migraine-rationale-and-progress
#16
Hsiangkuo Yuan, Clinton G Lauritsen, Eric A Kaiser, Stephen D Silberstein
Calcitonin gene-related peptide (CGRP), a neuropeptide abundant in the trigeminal system and widely expressed in both the peripheral and central nervous systems, has recently emerged as a promising target for migraine management. While known as a potent arterial vasodilator, the role of CGRP in migraine is likely mediated by modulating nociception and sustaining neurogenic inflammation that leads to further peripheral and central pain sensitization. Functional blockade of CGRP, which involves either CGRP receptor antagonists or monoclonal antibodies (mAbs) to CGRP or its receptor, has recently shown clinical efficacy in migraine management...
November 7, 2017: BioDrugs: Clinical Immunotherapeutics, Biopharmaceuticals and Gene Therapy
https://www.readbyqxmd.com/read/29059473/update-on-the-pharmacology-of-calcitonin-cgrp-family-of-peptides-iuphar-review-x
#17
REVIEW
Debbie L Hay, Michael L Garelja, David R Poyner, Christopher S Walker
The calcitonin/calcitonin gene-related peptide (CGRP) family of peptides includes calcitonin, α and β CGRP, amylin, adrenomedullin (AM) and adrenomedullin 2/intermedin (AM2/IMD). Their receptors consist of one of two G protein-coupled receptors (GPCRs), the calcitonin receptor (CTR) or the calcitonin receptor-like receptor (CLR). Further diversity arises from heterodimerisation of these GPCRs with one of three receptor activity-modifying proteins (RAMPs). This gives the CGRP receptor (CLR/RAMP1), the AM1 and AM2 receptors (CLR/RAMP2 or RAMP3) and the AMY1, AMY2 and AMY3 receptors (CTR/RAMPs1-3 complexes, respectively)...
October 23, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29023985/interaction-between-calcitonin-gene-related-peptide-immunoreactive-neurons-and-satellite-cells-via-p2y12-r-in-the-trigeminal-ganglion-is-involved-in-neuropathic-tongue-pain-in-rats
#18
Shiori Sugawara, Shinji Okada, Ayano Katagiri, Hiroto Saito, Tatsuro Suzuki, Hiroki Komiya, Kohei Kanno, Kinuyo Ohara, Toshimitsu Iinuma, Akira Toyofuku, Koichi Iwata
The P2Y12 receptor expressed in satellite cells of the trigeminal ganglion is thought to contribute to neuropathic pain. The functional interaction between neurons and satellite cells via P2Y12 receptors and phosphorylated extracellular signal-regulated kinase 1/2 (pERK1/2) underlying neuropathic pain in the tongue was evaluated in this study. Expression of P2Y12 receptor was enhanced in pERK1/2-immunoreactive cells encircling trigeminal ganglion neurons after lingual nerve crush. The administration to lingual nerve crush rats of a selective P2Y12 receptor antagonist, MRS2395, attenuated tongue hypersensitivity to mechanical and heat stimulation and suppressed the increase in the relative numbers of calcitonin gene-related peptide (CGRP)-immunoreactive neurons and neurons encircled by pERK1/2-immunoreactive cells...
October 11, 2017: European Journal of Oral Sciences
https://www.readbyqxmd.com/read/29019093/triptans-and-cgrp-blockade-impact-on-the-cranial-vasculature
#19
REVIEW
Silvia Benemei, Francesca Cortese, Alejandro Labastida-Ramírez, Francesca Marchese, Lanfranco Pellesi, Michele Romoli, Anne Luise Vollesen, Christian Lampl, Messoud Ashina
The trigeminovascular system plays a key role in the pathophysiology of migraine. The activation of the trigeminovascular system causes release of various neurotransmitters and neuropeptides, including serotonin and calcitonin gene-related peptide (CGRP), which modulate pain transmission and vascular tone. Thirty years after discovery of agonists for serotonin 5-HT1B and 5-HT1D receptors (triptans) and less than fifteen after the proof of concept of the gepant class of CGRP receptor antagonists, we are still a long way from understanding their precise site and mode of action in migraine...
October 10, 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28971699/cgrp-receptor-antagonist-mk-8825-attenuates-cortical-spreading-depression-induced-pain-behavior
#20
Aslı Filiz, Nermin Tepe, Sajedeh Eftekhari, H Evren Boran, Ergin Dilekoz, Lars Edvinsson, Hayrunnisa Bolay
Background and objective The present study aimed to investigate the effects of selective calcitonin gene related peptide (CGRP) receptor antagonist (MK-8825) on cortical spreading depression (CSD) induced pain behavior and anxiety in freely-moving rats, and neuronal activation in the correlated anatomical regions. Methods CSD was induced while keeping all meningeal layers and BBB intact and MK-8825 was administered in two different doses. Regional cerebral blood flow (rCBF), arterial pressure and DC shift were recorded...
January 1, 2017: Cephalalgia: An International Journal of Headache
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