Targeting a family B GPCR/RAMP receptor complex: CGRP receptor antagonists and migraine
نویسندگان
چکیده
منابع مشابه
Spinally mediated analgesic interaction between γ-aminobutyric acid B receptor agonist and glutamate receptor antagonists in rats
Background. Many mechanisms are involved in pain transmission in the spinal cord. Therefore, combination of drugs acting on different kinds of mechanisms might be useful for analgesia. We investigated the interaction betweenγ-aminobutyric acid (GABA)B receptor agonist, baclofen, and N-methyl-D-aspartate (NMDA) receptor antagonist, AP-5, orα-amino-3-hydroxy-5-methylisoxazole-4-propionic acid ...
متن کاملCGRP antagonists and antibodies for the treatment of migraine.
Introduction: Migraine is a highly devastating neurovascular disorder that affects up to 16% of the population worldwide. In spite of intensive research, its origin remains enigmatic with no therapeutic option appropriate for all migraine patients. One of the leading hypotheses is related to the function of the calcitonin gene-related peptide (CGRP). Regardless, the pharmaceutical options curre...
متن کاملFunctional and biophysical analysis of the C-terminus of the CGRP-receptor; a family B GPCR.
G-protein coupled receptors (GPCRs) typically have a functionally important C-terminus which, in the largest subfamily (family A), includes a membrane-parallel eighth helix. Mutations of this region are associated with several diseases. There are few C-terminal studies on the family B GPCRs and no data supporting the existence of a similar eighth helix in this second major subfamily, which has ...
متن کاملPreparation and preliminary biological evaluation of [153Sm] samarium AMD3100; towards a possible therapeutic chemokine receptor CXCR4 targeting complex
Introduction: In continuation of recent development of possible C-X-C chemokine receptor type 4 (CXCR4) imaging agents, we report the development of a possible CXCR4 targeted therapy agent. Methods: [153Sm]labeled 1,1′-[1,4-phenylenebis(methylene)] bis-1,4,8,11-tetraazacyclo -tetradecane ([153Sm]-AMD3100) was prepared using [153Sm]SmCl3 and AMD-3100 ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2012
ISSN: 0007-1188
DOI: 10.1111/j.1476-5381.2011.01633.x