Classification of Kinin Receptors
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Domenico Regoli
Abstract
This minireview is divided into three parts: the first part refers to the characterization and classification of kinin receptors using agonists and antagonists in isolated tissues (classical pharmacology). Two kinin receptors have been considered on the basis of their distinct pharmacology, namely the B1 receptor of the rabbit aorta (rank order of potency of agonists: LysdesArg9BK > desArg9BK >= LysBK>BK; apparent affinities of antagonists Lys[Leu8]desArg9BK (pIC50 8.4 ) > [Leu8]desArg9BK (pIC50 7.4)>>>HOE 140, a B2 receptor antagonist, pIC50<5.0), and the B2 receptor of the rabbit jugular vein (potency of agonists: LysBK = BK>>> LysdesArg9BK = desArg9BK and HOE 140 (pIC50 9.0)>>>Lys[Leu8]desArg9BK, pIC50<5.0). The second part describes speciesrelated B1receptor subtypes, demonstrated by different pharmacological profiles of agonists and antagonists: human, rabbit and pig subtypes (LysdesArg9BK >> desArg9B K and Lys[Leu8]desArg9BK > [Leu8]desArg9BK) and dog, rat, mouse and hamster B1 receptors (desArg9BK = LysdesArg9BK and [Leu8]desArg9BK = Lys[Leu8]desArg9BK). Affinities of agonists and antagonists in some species (man, rabbit, pig) are significantly increased (at least 10-fold) by the presence of a Lys at their Nterminus. The last part describes species-related B2 receptor subtypes supported by results obtained with non-peptide receptor agonists (FR 190997) and antagonists (FR 173657). While BK acts as a full agonist in man, rabbit and pig, FR 190997 behaves as a full agonist on human, as partial agonist on rabbit, and as pure antagonist on pig B2 receptors. Various hypotheses are considered to interpret these findings.
Copyright © 2001 by Walter de Gruyter GmbH & Co. KG
Articles in the same Issue
- To Our Authors, Readers and Subscribers
- Kinins 1925-2000
- The Expanded Human Kallikrein (KLK) Gene Family: Genomic Organisation, Tissue-Specific Expression and Potential Functions
- Novel Roles of Kallistatin, a Specific Tissue Kallikrein Inhibitor, in Vascular Remodeling
- Signal Transduction from Bradykinin, Angiotensin, Adrenergic and Muscarinic Receptors to Effector Enzymes, Including ADP-Ribosyl Cyclase
- Classification of Kinin Receptors
- Metabolism-Resistant Bradykinin Antagonists: Development and Applications
- Kinins, Receptors, Kininases and Inhibitors Where Did They Lead Us?
- Bradykinin Signalling to MAP Kinase: Cell-Specific Connections versus Principle Mitogenic Pathways
- Kinins and Epithelial Ion Transport in the Alimentary Tract
- Role of the Renal Kallikrein-Kinin System in the Development of Salt-Sensitive Hypertension
- Role of the Light Chain of High Molecular Weight Kininogen in Adhesion, Cell-Associated Proteolysis and Angiogenesis
- Activation of the Kinin-Forming Cascade on the Surface of Endothelial Cells
- Kallikrein and Kinin Receptor Expression in Inflammation and Cancer
- Altered Neutrophil Homeostasis in Kinin B1 Receptor-Deficient Mice
- Cystatins as Calpain Inhibitors: Engineered Chicken Cystatin- and Stefin B-Kininogen Domain 2 Hybrids Support a Cystatin-Like Mode of Interaction with the Catalytic Subunit of µ-Calpain
- Synthetic Peptides and Fluorogenic Substrates Related to the Reactive Site Sequence of Kunitz-Type Inhibitors Isolated from Bauhinia: Interaction with Human Plasma Kallikrein
- Identification and Characterization of an Aromatic Amino Acid Decarboxylase from the Filarial Nematode, Dirofilaria immitis
- Molecular Cloning and Pharmacological Characterization of the Canine B1 and B2 Bradykinin Receptors
- Ligand-Mediated Regulation of Kinin Receptors in the Rabbit
- Activation of Sphingosine Kinase by the Bradykinin B2 Receptor and Its Implication in Regulation of the ERK/MAP Kinase Pathway
Articles in the same Issue
- To Our Authors, Readers and Subscribers
- Kinins 1925-2000
- The Expanded Human Kallikrein (KLK) Gene Family: Genomic Organisation, Tissue-Specific Expression and Potential Functions
- Novel Roles of Kallistatin, a Specific Tissue Kallikrein Inhibitor, in Vascular Remodeling
- Signal Transduction from Bradykinin, Angiotensin, Adrenergic and Muscarinic Receptors to Effector Enzymes, Including ADP-Ribosyl Cyclase
- Classification of Kinin Receptors
- Metabolism-Resistant Bradykinin Antagonists: Development and Applications
- Kinins, Receptors, Kininases and Inhibitors Where Did They Lead Us?
- Bradykinin Signalling to MAP Kinase: Cell-Specific Connections versus Principle Mitogenic Pathways
- Kinins and Epithelial Ion Transport in the Alimentary Tract
- Role of the Renal Kallikrein-Kinin System in the Development of Salt-Sensitive Hypertension
- Role of the Light Chain of High Molecular Weight Kininogen in Adhesion, Cell-Associated Proteolysis and Angiogenesis
- Activation of the Kinin-Forming Cascade on the Surface of Endothelial Cells
- Kallikrein and Kinin Receptor Expression in Inflammation and Cancer
- Altered Neutrophil Homeostasis in Kinin B1 Receptor-Deficient Mice
- Cystatins as Calpain Inhibitors: Engineered Chicken Cystatin- and Stefin B-Kininogen Domain 2 Hybrids Support a Cystatin-Like Mode of Interaction with the Catalytic Subunit of µ-Calpain
- Synthetic Peptides and Fluorogenic Substrates Related to the Reactive Site Sequence of Kunitz-Type Inhibitors Isolated from Bauhinia: Interaction with Human Plasma Kallikrein
- Identification and Characterization of an Aromatic Amino Acid Decarboxylase from the Filarial Nematode, Dirofilaria immitis
- Molecular Cloning and Pharmacological Characterization of the Canine B1 and B2 Bradykinin Receptors
- Ligand-Mediated Regulation of Kinin Receptors in the Rabbit
- Activation of Sphingosine Kinase by the Bradykinin B2 Receptor and Its Implication in Regulation of the ERK/MAP Kinase Pathway
