Identification and characterization of B2 bradykinin receptors in sheep nasal turbinate membranes. 1990

R A Lyon, and P S Weisshaar, and R J Phipps
Procter and Gamble Co., Miami Valley Labs, Cincinnati, OH 45239.

Because bradykinin (BK) has been implicated as a mediator of upper respiratory tract symptomatology, specific 3H-BK binding was investigated in membrane homogenates prepared from sheep nasal turbinate tissue in order to identify and characterize the BK receptor subtype(s) present. 3H-BK saturation and Scatchard analyses revealed a single, high affinity, saturable site (KD of 0.098 nM) with a density of 0.44 pmol/g wet weight tissue. Competition experiments using B1 and B2 receptor agents revealed a B2-BK receptor pharmacology; the B2 agents BK, Lys-BK, NPC-567, [D-Phe7]-BK and [Thi,5,8 D-Phe7]-BK displayed nM affinity while the B1 agents [des-Arg9]-BK and [Leu,8 des-Arg9]-BK competed in the uM range. The absolute and rank order of affinities in this tissue paralleled that found in the guinea pig ileum. No specific binding was found using the putative B1 receptor radioligand 3H-[des-Arg9]-BK. Specific B2-BK receptor binding was not effected by the addition of non-hydrolyzable guanine or adenine nucleotides. These data confirm the presence of B2-BK receptors in this tissue and provide support for a role of BK in nasal function.

UI MeSH Term Description Entries
D008566 Membranes Thin layers of tissue which cover parts of the body, separate adjacent cavities, or connect adjacent structures. Membrane Tissue,Membrane,Membrane Tissues,Tissue, Membrane,Tissues, Membrane
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D001920 Bradykinin A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter. Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg,Bradykinin Acetate, (9-D-Arg)-Isomer,Bradykinin Diacetate,Bradykinin Hydrochloride,Bradykinin Triacetate,Bradykinin, (1-D-Arg)-Isomer,Bradykinin, (2-D-Pro)-Isomer,Bradykinin, (2-D-Pro-3-D-Pro-7-D-Pro)-Isomer,Bradykinin, (2-D-Pro-7-D-Pro)-Isomer,Bradykinin, (3-D-Pro)-Isomer,Bradykinin, (3-D-Pro-7-D-Pro)-Isomer,Bradykinin, (5-D-Phe)-Isomer,Bradykinin, (5-D-Phe-8-D-Phe)-Isomer,Bradykinin, (6-D-Ser)-Isomer,Bradykinin, (7-D-Pro)-Isomer,Bradykinin, (8-D-Phe)-Isomer,Bradykinin, (9-D-Arg)-Isomer,Arg Pro Pro Gly Phe Ser Pro Phe Arg
D005260 Female Females
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding
D012756 Sheep Any of the ruminant mammals with curved horns in the genus Ovis, family Bovidae. They possess lachrymal grooves and interdigital glands, which are absent in GOATS. Ovis,Sheep, Dall,Dall Sheep,Ovis dalli
D014420 Turbinates The scroll-like bony plates with curved margins on the lateral wall of the NASAL CAVITY. Turbinates, also called nasal concha, increase the surface area of nasal cavity thus providing a mechanism for rapid warming and humidification of air as it passes to the lung. Nasal Concha,Conchae Nasales,Conchae Nasale,Nasal Conchas,Turbinate
D017981 Receptors, Neurotransmitter Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses. Neurohumor Receptors,Neuromediator Receptors,Neuromodulator Receptors,Neuroregulator Receptors,Receptors, Neurohumor,Receptors, Synaptic,Synaptic Receptor,Synaptic Receptors,Neuromediator Receptor,Neuromodulator Receptor,Neuroregulator Receptor,Neurotransmitter Receptor,Receptors, Neuromediators,Receptors, Neuromodulators,Receptors, Neuroregulators,Receptors, Neurotransmitters,Neuromediators Receptors,Neuromodulators Receptors,Neuroregulators Receptors,Neurotransmitter Receptors,Neurotransmitters Receptors,Receptor, Neuromediator,Receptor, Neuromodulator,Receptor, Neuroregulator,Receptor, Neurotransmitter,Receptor, Synaptic,Receptors, Neuromediator,Receptors, Neuromodulator,Receptors, Neuroregulator
D018002 Receptors, Bradykinin Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself. Bradykinin Receptors,Bradykinin Receptor,Receptor, Bradykinin

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