Development of a binding assay for the B1 receptors for kinins
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Cited by (39)
Synthesis and evaluation of a<sup>68</sup>Ga-labeled bradykinin B1 receptor agonist for imaging with positron emission tomography
2017, Bioorganic and Medicinal ChemistryCitation Excerpt :Since Sar-[Hyp4,Cha6,d-Phe9,des-Arg10]kallidin was previously reported as a potent B1R agonist,31 our data showed that replacing Sar (sarcosine) with Ga-DOTA-Ahx did not change their agonist characteristics. In addition, our data also confirmed the reports by others that modification at the N-terminus of B1R-targeting peptides was tolerable without significantly affecting their binding affinities.32–34 To assess the stability of 68G-Z01115, both in vitro and in vivo studies were conducted and monitored by HPLC.
N-terminal extended conjugates of the agonists and antagonists of both bradykinin receptor subtypes: Structure-activity relationship, cell imaging using ligands conjugated with fluorophores and prospect for functionally active cargoes
2012, PeptidesCitation Excerpt :Maximakinin, a natural sequence isolated from amphibian skin, is composed of the full BK sequence at its C-terminal region with a 10-residue N-terminal extension (DLPKINRKGPRPPGFSPFR); this peptide has pharmacological activity in mammalian tissues [27,7] (see also Section 3.1.1). N-terminal extension of both agonist and antagonist B1R ligands is illustrated by development of the high affinity radioligand [125I]-Tyr-Gly-Lys-ɛ-aminocaproyl-Lys-des-Arg9-BK [22], successfully used in tumor autoradiography [25], or of the highly potent antagonist B-10324 (2,3,4,5,6-pentafluorocinnamoyl-B-9958) [16]. In this paper we review the properties of a series of recently produced and characterized kinin receptor ligands.
B-1 bradykinin receptor
2007, xPharm: The Comprehensive Pharmacology ReferenceDes-Arg<sup>9</sup>-bradykinin increases intracellular Ca<sup>2+</sup> in bronchoalveolar eosinophils from ovalbumin-sensitized and -challenged mice
2003, European Journal of PharmacologyKinin receptors: Functional aspects
2002, International Immunopharmacology