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.

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

Telcagepant potassium. Molecular Formula C 28 H 32 F 5 KN 6 O 4; Average mass 650.682 Da; Monoisotopic mass 650.204224 Da; ChemSpider ID 30791398 781649-09-0 - CGDZXLJGHVKVIE-DNVCBOLYSA-N - Telcagepant [USAN:INN] - Similar structures search, synonyms, formulas, resource links, and other chemical information. Olcegepant | C38H47Br2N9O5 | CID 6918509 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more. 953077-35-5 - VESUVMGLUABQCA-LEVQAPRMSA-M - Telcagepant potassium [USAN] - Similar structures search, synonyms, formulas, resource links, and other chemical information. Telcagepant blocks the binding of CGRP to receptors within the areas of the central and peripheral nervous system that are important for the transmission of migraine pain and thereby is believed to inhibit the transmission of pain signals that lead to migraine headaches. Telcagepant, also known as MK0974, is a calcitonin gene-related peptide receptor antagonist under development for the acute treatment and prevention of migraine. MedKoo Biosciences, Inc. Leading supplier of anticancer chemical reagents and kinase inhibitors Telcagepant It is an antagonist of the receptor for calcitonin gene-related peptide (CGRP), a primary neuropeptide involved in the pathophysiology of migraine.

Telcagepant (MK0974) is one of several calcitonin-gene-related peptide antagonists in development as a potential treatment for acute migraine attacks and is the first orally available drug in this For telcagepant, DILIsym predicted hepatotoxicity at clinical doses ≥ 175 mg BID, consistent with results from a phase 2 study for the acute treatment for migraine in which 13 of 638 people experienced ALT elevations ≥ 3× ULN, including 1.9% (5/258) of those treated with telcagepant 140 mg BID and 3.2% (8/253) of those treated with telcagepant 280 mg BID, compared with 0 of 127 people Telcagepant (MK-0974, Merck & Co., Inc.), an oral calcitonin gene-related peptide (CGRP) antagonist, is effective in treating acute migraine headache. Although CGRP receptor antagonists seem devoid of direct vasoconstrictor activity, animal research suggests a role for CGRP in nitroglycerin (NTG) induced vasodilation. Telcagepant for Prevention of Menstrually Related Migraine in Female Participants With Episodic Migraine (MK-0974-065) The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Structure and pharmacology of telcagepant The CGRP family of receptors mediate their physiological eﬀ ects through the joining of CLR and RAMP1, which are needed for G-protein signal transduction via the receptor component-protein.15 Initial high-throughput screening resulted in identiﬁ cation of a potent and orally bioavailable Importance of the field: Calcitonin gene-related peptide (CGRP) receptor antagonists have recently come to attention with the development of olcegepant and telcagepant for the treatment of migraine. The availability of high-affinity, non-peptide antagonists opens the way for trials of these compounds in other conditions where CGRP antagonism might be useful, such as septic shock and inhibition Overexpression of hRAMP1 increases CGRP signalling by changing the maximal response or ligand sensitivity, depending on tissue type. Furthermore, telcagepant inhibited transgenic hRAMP1 CGRP receptors, but the degree of inhibition suggests that the transgenic mice are only partially humanized or bot … Calcitonin gene-related peptide (CGRP) is a potent neuropeptide whose agonist interaction with the CGRP receptor (CGRP-R) in the periphery promotes vasodilation, neurogenic inflammation and trigeminovascular sensory activation.

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159 Starting from truncated analogs of olcegepant, they identified 165 (Fig. 36, K i = 280 nM) and optimized this flexible lead structure by incorporating conformational constraints.

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MedKoo Biosciences, Inc. Leading supplier of anticancer chemical reagents and kinase inhibitors Telcagepant (MK-0974) is a novel calcitonin gene-related peptide (CGRP) receptor antagonist currently undergoing clinical trials for migraine ().

9,10 This first report shows that 27% of patients respond to telcagepant whereas 33% of Sumatriptan patients respond and 40% of rizatriptan respond to being pain free after 2 h. 9 The second report, however, looked at the response rates of individuals that respond to triptans and those that do not.
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Telcagepant, also known as MK0974, is a calcitonin gene-related peptide receptor antagonist under development for the acute treatment and prevention of migraine. MedKoo Biosciences, Inc. Leading supplier of anticancer chemical reagents and kinase inhibitors Telcagepant (MK-0974) is a novel calcitonin gene-related peptide (CGRP) receptor antagonist currently undergoing clinical trials for migraine (). MK-0974 is currently being studied in phase III clinical trials. Telcagepant 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 migraine pain.

The availability of high-affinity, non-peptide antagonists opens the way for trials of these compounds in other conditions where CGRP antagonism might be useful, such as septic shock and inhibition Overexpression of hRAMP1 increases CGRP signalling by changing the maximal response or ligand sensitivity, depending on tissue type. Furthermore, telcagepant inhibited transgenic hRAMP1 CGRP receptors, but the degree of inhibition suggests that the transgenic mice are only partially humanized or bot … Calcitonin gene-related peptide (CGRP) is a potent neuropeptide whose agonist interaction with the CGRP receptor (CGRP-R) in the periphery promotes vasodilation, neurogenic inflammation and trigeminovascular sensory activation.
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Overexpression of hRAMP1 increases CGRP signalling by changing the maximal response or ligand sensitivity, depending on tissue type. Furthermore, telcagepant inhibited transgenic hRAMP1 CGRP receptors, but the degree of inhibition suggests that the transgenic mice are only partially humanized or bot …

781649-09-0 - CGDZXLJGHVKVIE-DNVCBOLYSA-N - Telcagepant [USAN:INN] - Similar structures search, synonyms, formulas, resource links, and other chemical information. Structure, properties, spectra, suppliers and links for: Telcagepant potassium, 953077-35-5. Telcagepant, also known as MK0974, is a calcitonin gene-related peptide receptor antagonist under development for the acute treatment and prevention of migraine. MedKoo Biosciences, Inc. Leading supplier of anticancer chemical reagents and kinase inhibitors Telcagepant (MK-0974) is a novel calcitonin gene-related peptide (CGRP) receptor antagonist currently undergoing clinical trials for migraine (). MK-0974 is currently being studied in phase III clinical trials. Telcagepant 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 migraine pain.