PILOCARPINE


Trade Names	OCUSERT PILO-20 OCUSERT PILO-40
Synonyms	Ocucarpine Ocusert pilo Ocusert pilo-20 Ocusert pilo-40 Pilocarpine Pilocarpinum Pilocarpol Pilokarpin Spersacarpine Syncarpine
Status
Molecule Category	Free-form
ATC	N07AX01 S01EB01
UNII	01MI4Q9DI3
EPA CompTox	DTXSID1021162


Active Pharmaceutical Ingredients Bioactive chemicals	Exact Similarity SubStructure	Threshold (%) >= 70


InChI Key	QCHFTSOMWOSFHM-WPRPVWTQSA-N
Smiles	CC[C@@H]1C(=O)OC[C@@H]1Cc1cncn1C
InChI	InChI=1S/C11H16N2O2/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2/h5,7-8,10H,3-4,6H2,1-2H3/t8-,10-/m0/s1

Mechanism of Action	Action	Reference
Muscarinic acetylcholine receptor M1 agonist	AGONIST	PubMed


Protein: Muscarinic acetylcholine receptor M1 Description: Muscarinic acetylcholine receptor M1 Organism : Homo sapiens P11229 ENSG00000168539










Protein: Muscarinic acetylcholine receptor M3 Description: Muscarinic acetylcholine receptor M3 Organism : Homo sapiens P20309 ENSG00000133019

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2A Cytochrome P450 2A6	-	-	3600	3000	-
Enzyme Cytochrome P450 Cytochrome P450 family 2 Cytochrome P450 family 2A	-	-	3000	1400	-
Membrane receptor Family A G protein-coupled receptor Small molecule receptor (family A GPCR) Monoamine receptor Acetylcholine receptor	18-8792	68-7600	2692-2692	83-3670	-
Transporter Electrochemical transporter SLC superfamily of solute carriers SLC22 family of organic cation and anion transporters	-	-	-	-	17

Assay Description	Organism	Bioactivity
Ability to displace [3H]cis--2-methyl-5-((dimethylamino)methyl)-1,3-di oxolane from muscarinic acetylcholine receptor in rat cortical tissue.	None	80.0 nM
Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue.	None	960.0 nM
Inhibition of [3H]OXO-M binding against muscarinic acetylcholine receptor in rat brain membranes	None	82.9 nM
Binding affinity against muscarinic acetylcholine receptor from rat brain crude membrane, using [3H]OXO-M (oxotremorine) as the radioligand.	None	26.0 nM
In vitro inhibition of [3H]Oxo-Mas binding to M1 and M4 receptors in rat brain homogenate.	None	67.0 nM
Binding affinity against muscarinic receptor in rat brain membranes using oxotremorine-M as ligand	None	68.0 nM
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy	Homo sapiens	17.0 %
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay	Homo sapiens	17.5 nM
Partial agonist activity at human muscarinic M1 acetylcholine receptor expressed in CHO cells assessed as increase in IP1 accumulation incubated for 30 mins by FRET based HTRF assay	Homo sapiens	831.76 nM

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