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Olcegepant
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Olcegepant
CAS No. : 204697-65-4
MCE 站:Olcegepant
产品活性:Olcegepant (BIBN-4096) 是有效和选择性的降钙素基因相关肽1 (CGRP1) 受体 拮抗剂,IC50 和 Ki 分别为0.03 nM,14.4 pM。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:CGRP Receptor
In Vitro: Olcegepant possesses higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology. Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM. Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment. Olcegepant (BIBN4096BS) exhibits competitive antagonism at the CGRP receptor present in SK-N-MC cells. Isolated human cerebral, coronary, and omental arteries are studied with a sensitive myograph technique. CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner.
In Vivo: Olcegepant (BIBN4096BS) in doses between 1 and 30 μg/kg (i.v.) inhibits the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys. Pre-treatment with Olcegepant (900 μg/kg) inhibits the capsaicin-induced expression of Fos throughout the spinal trigeminal nucleus by 57%. In contrast, the expression of phosphorylated extracellular signal-regulated kinase in the trigeminal ganglion is not changed by Olcegepant pre-treatment. Olcegepant (0.3 to 0.9 mg/kg, i.v.) markedly reduces mechanical allodynia in CCI-ION rats. Olcegepant (0.6 mg/kg, i.v.) significantly reduces the number of c-Fos immunolabeled cells in spinal nucleus of the trigeminal nerve and upregulation of ATF3 transcript (a marker of neuron injury) but not that of interleukin-6 in trigeminal ganglion of CCI-ION rats.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Calcitonin (salmon) | Rat CGRP-(8-37) | Olcegepant hydrochloride | Calcitonin Gene Related Peptide (CGRP) (83-119), rat TFA | β-CGRP, human TFA | Adrenomedullin (AM) (22-52), human | Ubrogepant | Calcitonin (human) | HCGRP-(8-37) | Adrenomedullin (11-50), rat | Adrenomedullin (16-31), human | Kendomycin | PHM-27 (human) | Adrenomedullin (1-50), rat | CGRP antagonist 1
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热门标签:BIBN-4096