Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0GB7C)
Name
Adenosine receptor A1 (AA1R)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Adenosine A1 receptor; Adenosine A1R; ADORA1
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name ADORA1 Gene ID
134
UniProt ID AA1R_HUMAN (click to find more protein-related data of this DBT)
TTD ID T92072 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT
PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM
VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL
FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL
KIWNDHFRCQPAPPIDEDLPEERPDD
Function
The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Receptor for adenosine.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Caffeine Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Other agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki > 10000 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID AA1R_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 130000 nM (tested by experiment) [2]
                   Tested Species Bos taurus (Bovine)
                   UniProt ID AA1R_BOVIN
             Experiment (3) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 100000 nM (tested by experiment) [3]
                   Tested Species Cavia porcellus (Guinea pig)
                   UniProt ID AA1R_CAVPO
             Experiment (4) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki > 10000 nM (tested by experiment) [1]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID AA1R_RAT
          DIG Name: Linoleic acid Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Penetration agent; Solubilizing agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 65000 nM (tested by experiment) [4]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID AA1R_RAT
References
1 Fluorescent-Labeled Selective Adenosine A 2B Receptor Antagonist Enables Competition Binding Assay by Flow Cytometry. J Med Chem. 2018 May 24; 61(10):4301-4316.
2 Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar; 25(3):197-207.
3 8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors. J Med Chem. 1992 Mar 6; 35(5):924-30.
4 Interference of linoleic acid fraction in some receptor binding assays. J Nat Prod. 1999 Jun; 62(6):912-4.

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