Bradykinin Receptor
The peptide kinins, of which the best known member is bradykinin, have long been established as important inflammatory mediators. Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domained family. The existence of two subtypes of bradykinin receptor, B 1 and B2. Kinins are synthesised de novo at sites of tissue damage, both peripherally and in the CNS, where they participate in the acute inflammatory response in the microvasculature and aid in tissue repair and healing. In addition, kinins have effects apparently unrelated to their roles as inflammatory mediators, including a possible role in the control of blood pressure. The majority of the actions of kinins are mediated via an interaction with cell surface bradykinin receptors.
Bradykinin receptors mediate the majority of the diverse documented biological actions of kinins, and many of the biological roles attributed to endogenous kinins. These include: contraction or relaxation of smooth muscle tone of the intestinal, urogenital and respiratory tracts, effects on epithelial ion transport, the circulation and blood presure, a putative transmitter role in the central nervous system and a modulatory role in control of cell function and mitogenesis. There is now a substantial body of evidence supporting a role for kinins in the pathophysiology of several inflammatory diseases, including pancreatitis, arthritis, cardiovascular disease, urinary tract disorders, upper and lower respiratory tract disorders including rhinitis and asthma, and in the pain and hyperalgesia that accompany inflammatory insult.
References
1.Hall JM,et al. Gen Pharmacol. 1997 Jan;28(1):1-6
Bradykinin receptors mediate the majority of the diverse documented biological actions of kinins, and many of the biological roles attributed to endogenous kinins. These include: contraction or relaxation of smooth muscle tone of the intestinal, urogenital and respiratory tracts, effects on epithelial ion transport, the circulation and blood presure, a putative transmitter role in the central nervous system and a modulatory role in control of cell function and mitogenesis. There is now a substantial body of evidence supporting a role for kinins in the pathophysiology of several inflammatory diseases, including pancreatitis, arthritis, cardiovascular disease, urinary tract disorders, upper and lower respiratory tract disorders including rhinitis and asthma, and in the pain and hyperalgesia that accompany inflammatory insult.
References
1.Hall JM,et al. Gen Pharmacol. 1997 Jan;28(1):1-6
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(471)
Bombesin Receptor(11)
Bradykinin Receptor(18)
Calcium Channel(137)
cAMP(9)
Cannabinoid Receptor(69)
CaSR(17)
CGRP Receptor(14)
Chemokine Receptor(104)
Cholecystokinin Receptor(17)
CRF Receptor(13)
Dopamine Receptor(145)
Endothelin Receptor(20)
FFAR(5)
Galanin Receptor(1)
GHSR(16)
Glucagon Receptor(36)
GPCR19(7)
GPR119(3)
Hedgehog (Hh)(27)
Histamine Receptor(110)
Imidazoline Receptor(1)
Leukotriene Receptor(9)
LHR(1)
LPA Receptor(12)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(6)
Melanocortin Receptor(22)
Melatonin Receptor(5)
mGluR(11)
Motilin Receptor(4)
Neurokinin Receptor(34)
Neuropeptide Y Receptor(36)
Neurotensin Receptor(8)
Orexin Receptor(14)
Other Targets(3)
OXTR(2)
P2Y Receptor(8)
PAR(24)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(60)
PTH Receptor(1)
S1P Receptor(22)
SGLT(22)
Somatostatin Receptor(11)
Urotensin Receptor(4)
Vasopressin Receptor(16)
Bradykinin Receptor
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[Phe8Ψ(CH-NH)-Arg9]-Bradykinin
catalog no : M30746
cas no: 118122-39-7
Selective bradykinin B2 receptor agonist that is resistant to carboxypeptidase cleavage. 5-fold more potent and exhibits a more prolonged duration of action than bradykinin in vivo. -
Lys-[Des-Arg9]Bradykinin
catalog no : M30745
cas no: 71800-36-7
Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin. -
Sar-[D-Phe8]-des-Arg9-Bradykinin
catalog no : M30744
cas no: 126959-88-4
Potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo. -
Bombinakinin M
catalog no : M30743
cas no: 509151-65-9
Potent bradykinin receptor agonist. Highly selective for mammalian arterial smooth muscle bradykinin receptors, displaying ~ 50-fold greater potency than bradykinin. Elicits dose-dependent contractile effects in smooth muscle of guinea pig ileum (EC50 = 4.0 nM). -
MEN 11270
catalog no : M30640
cas no: 235082-52-7
Peptide antagonist of the B2 bradykinin receptor (pKi = 10.3); conformationally constrained cyclized analog of HOE 140. Blocks hypotension and bronchoconstriction in vivo. Displays selectivity for B2 over 29 other receptors and ion channels (pIC50 < 5.5).