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| Formula | C23H40N2O4 |
| Molar mass | 408.583 g·mol−1 |
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Capsinolol is a beta blocker derived from nonivamide. It is the first beta blocker with an associated calcitonin gene-related peptide releasing activity in the heart. [1]
Calcitonin is a 32 amino acid peptide hormone secreted by parafollicular cells (also known as C cells) of the thyroid gland in humans, and in many other animals in the ultimopharyngeal body. It acts to reduce blood calcium (Ca2+), opposing the effects of parathyroid hormone (PTH).
In pharmacology, an inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
Amylin, or islet amyloid polypeptide (IAPP), is a 37-residue peptide hormone. It is cosecreted with insulin from the pancreatic β-cells in the ratio of approximately 100:1 (insulin:amylin). Amylin plays a role in glycemic regulation by slowing gastric emptying and promoting satiety, thereby preventing post-prandial spikes in blood glucose levels.
Neurogenic inflammation is inflammation arising from the local release by afferent neurons of inflammatory mediators such as Substance P, Calcitonin Gene-Related Peptide (CGRP), neurokinin A (NKA), and endothelin-3 (ET-3). In such neurons, release of these pro-inflammatory mediators is thought to be triggered by the activation of ion channels that are the principal detectors of noxious environmental stimuli. In particular, the heat/capsaicin receptor TRPV1 and the irritant/wasabi receptor TRPA1. TRPA1 channels stimulated by lipopolysaccharide (LPS) may also cause acute neurogenic inflammation. Once released, these neuropeptides induce the release of histamine from adjacent mast cells. In turn, histamine evokes the release of substance P and calcitonin gene-related peptide; thus, a bidirectional link between histamine and neuropeptides in neurogenic inflammation is established.
Calcitonin gene-related peptide (CGRP) is a member of the calcitonin family of peptides, which in humans exists in two forms: α-CGRP and β-CGRP, also known as CGRP I and CGRP II. CGRP I or α-CGRP is a 37-amino acid neuropeptide and is formed from the alternative splicing of the calcitonin/CGRP gene located on chromosome 11. CGRP II or β-CGRP is less studied. In humans, β-CGRP differs from the α-CGRP by three amino acids and is encoded in a separate gene within the same vicinity. The CGRP family includes calcitonin (CT), adrenomedullin (AM), and amylin (AMY). This article outlines the basic function of CGRP as well as sources of production and synthesis. It further introduces receptors and regulation of CGRP, with a focus on human and mammalian systems.
Adrenomedullin is a vasodilator peptide hormone of uncertain significance in human health and disease. It was initially isolated in 1993 from a pheochromocytoma, a tumor of the adrenal medulla: hence the name.
Receptor activity modifying protein 1 is a protein that in humans is encoded by the RAMP1 gene.
Receptor activity modifying protein 2, also known as RAMP2, is a protein which in humans is encoded by the RAMP2 gene.
Receptor activity modifying protein 3, also known as RAMP3, is a human gene.
Calcitonin receptor-like (CALCRL), also known as the calcitonin receptor-like receptor (CRLR), is a human protein; it is a receptor for calcitonin gene-related peptide.
DNA-directed RNA polymerase III subunit RPC9 is an enzyme that in humans is encoded by the CRCP gene.
ADM2 is a protein that in humans is encoded by the ADM2 gene.
In molecular biology, the amylin protein family or calcitonin/CGRP/IAPP protein family is a family of proteins, which includes the precursors of calcitonin/calcitonin gene-related peptide (CGRP), islet amyloid polypeptide (IAPP) and adrenomedullin.
Zucapsaicin (Civanex) is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. Zucapsaicin is a member of phenols and a member of methoxybenzenes It is a modulator of transient receptor potential cation channel subfamily V member 1 (TRPV-1), also known as the vanilloid or capsaicin receptor 1 that reduces pain, and improves articular functions. It is the cis-isomer of capsaicin. Civamide, manufactured by Winston Pharmaceuticals, is produced in formulations for oral, nasal, and topical use.
Calcitonin gene-related peptide (CGRP) receptor antagonists are a class of drug candidates that act as antagonists of the calcitonin gene-related peptide receptor (CGRPR).
Neuroendocrine differentiation is a term primarily used in relation to prostate cancers that display a significant neuroendocrine cell population on histopathological examination. These types of prostate cancer comprise true neuroendocrine cancers, such as small cell carcinoma, carcinoid and carcinoid-like tumors, as well as prostatic adenocarcinoma exhibiting focal neuroendocrine phenotype.
Eptinezumab, sold under the brand name Vyepti, is a medication for the preventive treatment of migraine in adults. It is a monoclonal antibody that targets calcitonin gene-related peptides (CGRP) alpha and beta. It is administered by intravenous infusion every three months.
Erenumab, sold under the brand name Aimovig, is a medication which targets the calcitonin gene-related peptide receptor (CGRPR) for the prevention of migraine. It was the first of the group of CGRPR antagonists to be FDA approved in 2018. It is a form of monoclonal antibody therapy in which antibodies are used to block the receptors for the protein CGRP, thought to play a major role in starting migraines.
Fremanezumab, sold under the brand name Ajovy, is a medication used to prevent migraines in adults. It is given by injection under the skin.
Iain Macintyre FRS was a British endocrinologist who made important contributions to the understanding of calcium regulation and bone metabolism. Shortly after the hormone calcitonin had been described by Harold Copp, Macintyre's team was the first to isolate and sequence the hormone and to demonstrate its origin in the parafollicular cells of the thyroid gland. He subsequently analysed its physiological actions. Along with H. R. Morris he isolated and sequenced calcitonin gene-related peptide. Later research centred on the role played by nitric oxide on bone metabolism.
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