Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0N6ZL)
Name
Muscarinic receptor M2 (ACM2)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Muscarinic acetylcholine receptor M2; Cholinergic receptor, muscarinic 2; M2R; M2 receptor; CHRM2; Chrm2; Cholinergic/acetylcholine receptor M2
Family G-protein coupled receptor (GPCR)  >>  G-protein coupled rhodopsin receptor (GPCR-A)
Organism
Homo sapiens (Human)
Gene Name CHRM2 Gene ID
1129
UniProt ID ACM2_HUMAN (click to find more protein-related data of this DBT)
TTD ID T46185 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNY
FLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFD
RYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQF
FSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRI
VKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDE
ITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNI
VARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNT
VWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR
Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then triggers calcium ion release into the cytosol.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Cetylpyridinium chloride 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
Antimicrobial preservative; Penetration agent; Solubilizing agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 0.8 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM2_HUMAN
          DIG Name: D&C red no. 28 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 0.68 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM2_HUMAN
          DIG Name: Benzethonium chloride 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
Antimicrobial preservative; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1.1 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM2_HUMAN
          DIG Name: Methylene blue 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 0.19 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM2_HUMAN
          DIG Name: Methylpyrrolidone 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
Penetration agent; Solubilizing agent; Solvent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity Ki = 1600 nM (estimated based on the structural similarity with CHEMBL41779 ) [2]
                   Structural Similarity Tanimoto coefficient = 0.87804878
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID ACM2_RAT
          DIG Name: FD&C red no. 3 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
Colorant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 0.8 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM2_HUMAN
          DIG Name: Polysorbate 80 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; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 1.3 uM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID ACM2_HUMAN
References
1 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
2 The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives. J Med Chem. 1993 Nov 12; 36(23):3533-41.

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