Target Validation Information
Target ID T93509
Target Name Calcitonin gene-related peptide 1
Target Type
Clinical Trial
Drug Potency against Target Ac-WVTH[Cit]LAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2 Drug Info IC50 = 8.9 nM [529839]
Ac-WVTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2 Drug Info IC50 = 0.2 nM [529839]
Ac-WVTH[Cit]LAGLLSRSGGVVRKNFVPTDVGPFAF-NH2 Drug Info IC50 = 0.57 nM [529839]
Gamma Hydroxybutyric Acid Drug Info IC50 = 0.24 nM [552753]
Ac-WVEHRLKGELSRKGGVV[hArg]KNFVPTDVGPFAF-NH2 Drug Info IC50 = 1.02 nM [529839]
VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2 Drug Info IC50 = 4.87 nM [529839]
Ac-WVTH[hArg]LAGLLS[hArg]SGGVVRKNFVPTDVGPFAF-NH2 Drug Info IC50 = 20.4 nM [529839]
Ac-VTHRLAGLLSRSGGVVRKNFVPTDVGPFAF-NH2 Drug Info IC50 = 0.71 nM [529839]
Ac-WVTHQLAGLLSQSGGVVRKNFVPTDVGPFAF-NH2 Drug Info IC50 = 0.53 nM [529839]
Ac-VTHRLAGLLSRSGGVVKNNFVPTDVGPFAF-NH2 Drug Info IC50 = 1.74 nM [529839]
FV-Aib-TDVGPFAF Drug Info IC50 = 740 nM [529839]
WVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF-NH2 Drug Info IC50 = 0.64 nM [529839]
Ac-WVTHRLAGLLS[Cit]SGGVVRKNFVPTDVGPFAF-NH2 Drug Info IC50 = 0.58 nM [529839]
Action against Disease Model Olcegepant In an in vivo model, BIBN4096BS in doses between 1 and 30 micrograms kg-1 (i.v.) inhibited the effects of CGRP, released by stimulation of the trigeminal ganglion, on facial blood flow in marmoset monkeys [552216] Drug Info
The Effect of Target Knockout, Knockdown or Genetic Variations The use of CGRP knockout mice has let to characterize the endogenous role of CGRP showing that the local release of this neuropeptide protects from ethanol injury and favours ulcer healing. Decreased levels of gastric CGRP-like immunoreactivity (li) were observed during acetic acid-, cysteamine-, concentrated ethanol- or water immersion stress-ulcers. Restoration of CGRP-li was found in animals bearing ulcers in healing status and delayed healing in mice knockout to CGRP. CGRP was able to release somatostatin from gastric D cells but its main effects on the stomach homeostasis rely on local vasodilator action during increased acid-back diffusion. [529839]
References
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 552753Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Curr Opin Pharmacol. 2007 Dec;7(6):583-92. Epub 2007 Nov 9.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 529839J Med Chem. 2008 Dec 25;51(24):7889-97.Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor.
Ref 552216Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3.

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