About: Evidence for the existence of two forms of α(2A)-adrenoceptors in the rat

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About: Evidence for the existence of two forms of α(2A)-adrenoceptors in the rat Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : covidontheweb.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Evidence for the existence of two forms of α(2A)-adrenoceptors in the rat
Creator	Lien, Eric Chhajlani, Vijay Wikberg, Jarl Uhl6n, Staffan Xia, Yun
Source	PMC
abstract	The α(2A)-adrenoceptors in rat spleen, kidney, spinal cord and cerebral cortex were studied using [(3)H]-RX821002 radioligand binding. In the spleen, spinal cord and cerebral cortex, the ligand bound to saturable sites with a K (d) of about 1 nmol/l and capacities of 134, 240 and 290 fmol/mg protein, respectively. Computer modelling competition curves for 39 drugs, including those for α(2A)-, α(2B)- or α(2C)-adrenoceptor selective drugs, indicated that the sites labelled by [(3)H]-RX821002 in the spleen consisted of a single population of α(2A)-adrenoceptors. However, the competition curves for guanoxabenz were definitely biphasic and resolved into two site fits, indicating that guanoxabenz was binding to both high affinity (K (d) = 35 nmol/1) and low affinity (K (d) = 8900 nmol/1) α(2A)-adrenoceptor sites in the proportions 57% and 43%, respectively. The K (d) (S)for a number of α(2)-adrenoceptor subtype selective drugs, measured in competition with [(3)H]-RX821002 in cerebral cortex and spinal cord, were highly correlated with those obtained in the spleen indicating their α(2A)-adrenoceptor nature. However, by contrast to the results with the spleen, the guanoxabenz competition curves for the spinal cord and cerebral cortex were monophasic and resolved only into one site fits, the K (d) of guanoxabenz being about 4000 nmol/l for both tissues. Drug K (d) (S)for kidney α(2A)-adrenoceptors were also determined using [(3)H]-RX821002. For nearly all drugs tested, the K (d) (S)were highly correlated with those found for the α(2A)-adrenoceptors in the other rat tissues. However, for guanoxabenz, the data indicated that it competed with [(3)H]-RX821002 at a single α(2A)-adrenoceptor site with a K (d) of 39 nmol/1. When the rat α(2A)-adrenoceptor gene RG20 was transiently expressed in COS-7 cells and its ligand binding properties probed using [(3)H]-RX821002, the drug K (d) (S)obtained were also highly correlated with those found for the α(2A)-adrenoceptors in the spleen, cerebral cortex, spinal cord and kidney of the rat. For the RG20 encoded receptor, the guanoxabenz competition curves were steep and monophasic and modelled best into one site fits, with the Kd of guanoxabenz being 5200 nmol/1. It is suggested that guanoxabenz can differentiate between two forms of α(2A)-adrenoceptors in the rat: α(2A1) and α(2A2). The α(2A1)-form is present in the spleen and kidney where it shows a high apparent affinity for guanoxabenz. The α(2A2)-form shows a low apparent affinity for guanoxabenz and is present in the spleen, cerebal cortex and spinal cord. The α(2A2)-form of the rat α(2)-adrenoceptor appears to be encoded by the RG20 gene. The α(2A), and α(2A2)-adrenoceptor forms do not represent high and low affinity receptor forms for agonists because assays included EDTA, Gpp(NH)p and Na(+), which eliminated the high affinity receptors for agonists.
has issue date	1993-01-01(xsd:dateTime)
bibo:doi	10.1007/bf00167446
bibo:pmid	8097566
has license	no-cc
sha1sum (hex)	01c9dcd5cdb878c778dc7dbced9945c3b9ca8a42
schema:url	https://doi.org/10.1007/bf00167446
resource representing a document's title	Evidence for the existence of two forms of α(2A)-adrenoceptors in the rat
has PubMed Central identifier	PMC7087569
has PubMed identifier	8097566
schema:publication	Naunyn Schmiedebergs Arch Pharmacol
resource representing a document's body	covid:01c9dcd5cdb878c778dc7dbced9945c3b9ca8a42#body_text
is schema:about of	named entity 'EVIDENCE FOR' named entity 'existence' named entity 'A2A' named entity 'FORMS' named entity 'PHARMACOLOGY' named entity 'ADRENOCEPTORS' named entity 'RAT' named entity 'biphasic' named entity 'Imperial Chemical Industries' named entity 'guanoxabenz' named entity 'spinal cord' named entity 'quinoxaline' named entity 'protein' named entity 'Boehringer Ingelheim' named entity '1.6' named entity 'adrenoceptors' named entity 'COS-7 cells' named entity 'rat' named entity 'guanoxabenz' named entity 'kidney' named entity 'kidney' named entity 'receptor' named entity 'dopamine' named entity 'oxymetazoline' named entity 'kidney' named entity 'agonist' named entity 'guanoxabenz' named entity 'spinal cord' named entity 'EDTA' named entity 'plasmid DNA' named entity 'cerebral cortex' named entity 'high affinity' named entity 'spinal cord' named entity 'oxymetazoline' named entity 'pKi' named entity 'guanoxabenz' named entity 'EDTA' named entity 'cloned' named entity 'imidazol' named entity 'adrenoceptors' named entity 'Radioligand binding' named entity 'oxymetazoline' named entity 'guanoxabenz' named entity 'adrenoceptor' named entity 'EDTA' named entity 'high affinity' named entity 'agonist' named entity 'rat' named entity 'biphasic' named entity 'adrenoceptors' named entity 'yohimbine' named entity 'adrenoceptor' named entity 'Non-specific' named entity 'cerebral cortex' named entity 'PKi' named entity 'guanoxabenz' named entity 'adrenoceptor' named entity 'spinal cord' named entity 'gene' named entity 'France' named entity 'guanoxabenz' named entity 'guanoxabenz' named entity 'adrenoceptors' named entity 'adrenoceptor' named entity 'adrenoceptors' named entity 'rat' named entity 'guanoxabenz' named entity 'SKF' named entity 'kidney' named entity 'COS-7' named entity 'adrenoceptors' named entity 'cerebral cortex' named entity 'pharmacological properties' named entity 'ethyl' named entity 'spleen' named entity 'methyl' named entity 'spinal cord'

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