Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0HP4F)
Name
Cannabinoid CB1 receptor (CNR1)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Cannabinoid receptor 1; Brain-type cannabinoid receptor; CANN6; CB-R; CANN6; CB-R; CB1; CNR
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name CNR1 Gene ID
1268
UniProt ID CNR1_HUMAN (click to find more protein-related data of this DBT)
TTD ID T76685 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA
VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF
HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM
WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK
AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL
AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ
PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
Function
Mediates many cannabinoid-induced effects, acting, among others, on food intake, memory loss, gastrointestinal motility, catalepsy, ambulatory activity, anxiety, chronic pain. Signaling typically involves reduction in cyclic AMP. In the hypothalamus, may have a dual effect on mitochondrial respiration depending upon the agonist dose and possibly upon the cell type. Increases respiration at low doses, while decreases respiration at high doses.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Oleth-2 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; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 39810.72 nM (estimated based on the structural similarity with CHEMBL200113 ) [1]
                   Structural Similarity Tanimoto coefficient = 0.793103448
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID CNR1_RAT
          DIG Name: Tricaprilin 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
Dispersing agent; Emollient; Lubricant; Penetration agent; Plasticizing agent; Solubilizing agent; Solvent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki > 1000 nM (estimated based on the structural similarity with CHEMBL26440 ) [2]
                   Structural Similarity Tanimoto coefficient = 1
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID CNR1_RAT
          DIG Name: Xipamide 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
Ointment base
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 199.53 nM (estimated based on the structural similarity with CHEMBL246302 ) [3]
                   Structural Similarity Tanimoto coefficient = 0.82010582
                   Tested Species Homo sapiens (Human)
                   UniProt ID CNR1_HUMAN
References
1 3D-QSAR studies on cannabinoid CB1 receptor agonists: G-protein activation as biological data. J Med Chem. 2006 Jan 26; 49(2):554-66.
2 Assay and inhibition of diacylglycerol lipase activity. Bioorg Med Chem Lett. 2012 Jul 15; 22(14):4585-92.
3 Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies. Bioorg Med Chem Lett. 2007 Jan 1; 17(1):272-7.

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