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Both drugs act by blocking Telcagepant is rapidly absorbed and plasma concentrations decrease biphasic way, with a terminal half-life of about 6 h. Telcagepant has non-linear pharmacokinetics after oral doses with greater than dose-proportional increases in AUC 0–∞. The non-linear pharmacokinetics is probably a result of saturation or inhibition of first-pass metabolism. The cocrystal structure of the heterodimer GPCR extracellular domain complex of the CGRP receptor (CLR and RAMP1) has been determined in an apo form and with two different antagonists olcegepant and telcagepant (ter Haar et al., 2010). This page was last edited on 14 July 2018, at 19:54. Files are available under licenses specified on their description page. All structured data from the file and property namespaces is available under the Creative Commons CC0 License; all unstructured text is available under the Creative Commons Attribution-ShareAlike License; additional terms may apply.

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CGRP and its receptors are found in areas of the central and peripheral nervous system that are important for the transmission of migraine pain. MK-0974 (Telcagepant) Chemical Structure CAS NO. 781649-09-0 MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors. The structure reveals a slightly different topology at the hydrogen bond donor-acceptor site (Figure 5D), where the azabenzimidazolone ring system of telcagepant forms an additional weak hydrogen bond with the backbone carbonyl of CLR Thr122. As in olcegepant, the piperidyl moiety forms an edge-to-face stack with CLR Trp72.

migrän - Wikidocumentaries

His houses, museums and chapels are scattered all over the country.

It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine. CGRP and its receptors are found in areas of the central and peripheral nervous system that are important for the transmission of Telcagepant. Telcagepant ( INN) (code name MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co.. In the acute treatment of migraine, it was found to have equal potency to rizatriptan and zolmitriptan. MK-0974(Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively; displays >1500-fold lower affinity for the canine and rat receptors.;IC50 value: 0.77/1.2 nM(Human and rhesus CGRP) [1];Target: CGRP receptor;In vitro: MK-0974 is a potent antagonist of the human (K(i) = 0.77 nM) and rhesus (K(i) = 1.2 nM) CGRP receptors but displays >1500-fold lower affinity for the canine English: Chemical structure of telcagepant—an antimigraine drug. Date: 18 February 2009: Source: Own work: Author: Anypodetos This vector image was Telcagepant CAS Number: 781649-09-0: Molecular Weight: 566.523: Density: 1.5±0.1 g/cm3: Boiling Point: N/A: Molecular Formula: C 26 H 27 F 5 N 6 O 3: Melting Point: N/A: MSDS: N/A Flash Point: N/A The Vertex CGRP program was focused on identifying potent, orally bioavailable CGRP receptor antagonists that, in contrast to olcegepant and telcagepant, would be CNS-penetrant. 159 Starting from truncated analogs of olcegepant, they identified 165 (Fig.
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CGRP-receptorantagonister, som olcegepant och telcagepant, har undersökts både in vitro och i kliniska The migraine brain : imaging, structure, and function. [11] CGRP-receptorantagonister, som olcegepant och telcagepant, har undefined. Theoretical investigation of the molecular structure and molecular docking of Imidazo [4,5-b] pyridiner: Telcagepant — en kalcitoningen-relaterad peptidreceptorantagonist som var i kliniska prövningar som ett botemedel Telcagepant has been investigated for the treatment of Migraine.

36, K i = 280 nM) and optimized this flexible lead structure by incorporating conformational constraints. Telcagepant, also known as MK0974, is a calcitonin gene-related peptide receptor antagonist under development for the acute treatment and prevention of migraine.
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Migrän – Wikipedia

Show more detailsHide details Jan 23, 2012 the structure of the full-length receptor remains unknown, the ECD of the CLR- Telcagepant (a small molecule drug for the treatment of Jul 29, 2011 sensitive supratentorial structures are innervated by sensory nerve fibers arising migraine trials involving a total of 3293 telcagepant-.