3H-yohimbine binding to guinea-pig kidney and calf cerebral cortex membranes: comparison with human platelets. 1983

O E Brodde, and T Eymer, and J Arroyo

The highly specific alpha 2-adrenoceptor antagonist 3H-yohimbine was used to label in guinea-pig kidney and calf cerebral cortex membranes alpha 2-adrenoceptors. In both tissues binding was saturable, of high affinity (KD = 3-5 nM), rapid and readily reversible. alpha-Adrenergic antagonists inhibited binding with rank order of potency: rauwolscine greater than or equal to yohimbine greater than phentolamine much greater than prazosin greater than or equal to corynanthine, which is the typical one for alpha 2-adrenoceptors. Displacement curves of alpha-adrenergic agonists (clonidine greater than guanfacine greater than adrenaline greater than or equal to noradrenaline) were in the absence of GTP shallow with pseudo-Hill coefficients (nH) significantly less than 1.0. In the presence of GTP (10(-4) M) the curves were shifted to the right to lower affinities. However, only in guinea-pig kidney membranes nH increased up to 1.0, while in calf cerebral cortex membranes nH was not significantly influenced by GTP. The properties of alpha 2-adrenoceptors--as assessed by 3H-yohimbine binding--in guinea-pig kidney and calf cerebral cortex are, therefore, very similar to those recently determined under identical experimental conditions in human platelet membranes (Brodde et al., 1982). Although some tissue and/or species differences exist--especially the 5-6 times higher affinity of prazosin at renal and brain than at platelet alpha 2-adrenoceptors--it is concluded that alterations of human platelet alpha 2-adrenoceptors under various (patho) physiological conditions can be taken as representative for changes of other peripheral and/or central alpha 2-adrenoceptors.

UI MeSH Term Description Entries
D007668 Kidney Body organ that filters blood for the secretion of URINE and that regulates ion concentrations. Kidneys
D007700 Kinetics The rate dynamics in chemical or physical systems.
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
D011942 Receptors, Adrenergic, alpha One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation. Adrenergic alpha-Receptor,Adrenergic alpha-Receptors,Receptors, alpha-Adrenergic,alpha-Adrenergic Receptor,alpha-Adrenergic Receptors,Receptor, Adrenergic, alpha,Adrenergic alpha Receptor,Adrenergic alpha Receptors,Receptor, alpha-Adrenergic,Receptors, alpha Adrenergic,alpha Adrenergic Receptor,alpha Adrenergic Receptors,alpha-Receptor, Adrenergic,alpha-Receptors, Adrenergic
D001792 Blood Platelets Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation. Platelets,Thrombocytes,Blood Platelet,Platelet,Platelet, Blood,Platelets, Blood,Thrombocyte
D002417 Cattle Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor. Beef Cow,Bos grunniens,Bos indicus,Bos indicus Cattle,Bos taurus,Cow,Cow, Domestic,Dairy Cow,Holstein Cow,Indicine Cattle,Taurine Cattle,Taurus Cattle,Yak,Zebu,Beef Cows,Bos indicus Cattles,Cattle, Bos indicus,Cattle, Indicine,Cattle, Taurine,Cattle, Taurus,Cattles, Bos indicus,Cattles, Indicine,Cattles, Taurine,Cattles, Taurus,Cow, Beef,Cow, Dairy,Cow, Holstein,Cows,Dairy Cows,Domestic Cow,Domestic Cows,Indicine Cattles,Taurine Cattles,Taurus Cattles,Yaks,Zebus
D002540 Cerebral Cortex The thin layer of GRAY MATTER on the surface of the CEREBRAL HEMISPHERES that develops from the TELENCEPHALON and folds into gyri and sulci. It reaches its highest development in humans and is responsible for intellectual faculties and higher mental functions. Allocortex,Archipallium,Cortex Cerebri,Cortical Plate,Paleocortex,Periallocortex,Allocortices,Archipalliums,Cerebral Cortices,Cortex Cerebrus,Cortex, Cerebral,Cortical Plates,Paleocortices,Periallocortices,Plate, Cortical
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
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

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