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Drug-Target Interaction

Drug

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PubChem ID:5909
Structure:
Synonyms:
(+)-Pilocarpine hydrochloride
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-one hydrochloride
(3S,4R)-4,5-Dihydro-3-ethyl-4-(1-methyl-1H-imidazol-5-ylmethyl)-2(3H)-furanone hydrochloride
2(3H)-Furanone, 3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-,
2(3H)-Furanone, 3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-, monohydrochloride, (3S,4R)-
2(3H)-Furanone, 3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-, monohydrochloride, (3S-cis)-
2(3H)-Furanone, 3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-, monohydrochloride, (3S-cis)-
54-71-7
Adsorbocarpine
AI3-61859
Akarpine
Almocarpine
Ami-pilo
Amistura P
BETOPTIC PILO
C11H16N2O2.HCl
component of E-Pilo
component of Epicar
component of Pilocar
CPD000059053
D02200
E-Pilo
EINECS 200-212-5
Epicar
EU-0100950
Isopto carpine
Isopto carpine (TN)
Isopto P-ES
Isopto-carpine
Isoptocarpine
LS-109779
Mi-Pilo
MI-Pilo Ophth Sol
Mistura P
Mixture Name
MLS000069454
MLS000758210
MLS001076314
NCGC00094254-01
NSC 5746
NSC5746
P0472_SIGMA
P6503_SIGMA
PILO
Pilocar
Pilocar SMP
Pilocarpal
Pilocarpine chloride
Pilocarpine HCl
Pilocarpine hydrochloride
Pilocarpine hydrochloride (JP15/USP)
Pilocarpine hydrochloride [USAN:JAN]
Pilocarpine monohydrochloride
Pilocarpine muriate
Pilocarpine, hydrochloride
PILOCARPINE, MONOHYDROCHLORIDE
Pilocel
Pilokarpin monohydrochloride
Pilomiotin
Pilopine HS
Pilopine HS (TN)
Pilopine HS Gel
Pilovisc
Salagen
SAM001246962
Sanpilo
Sanpilo (TN)
SBB006456
SMR000059053
Sno pilo
Spersacarpine hydrochloride
WLN: T5OVTJ C2 D1- DT5N CNJ C1 &GH

Target

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Uniprot ID:ACM4_HUMAN
Synonyms:
Muscarinic acetylcholine receptor M4
EC-Numbers:-
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

16002459
Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor.. Marianne K O Grant; Esam E El-Fakahany (2005) The Journal of pharmacology and experimental therapeutics display abstract
Xanomeline is a functionally selective M1/M4 muscarinic acetylcholine receptor agonist. We have previously identified a novel mode of interaction of this ligand with the muscarinic M1 receptor that involves persistent binding and activation of the receptor after extensive washout. In the present study, we tested the hypothesis that xanomeline also binds in a wash-resistant manner to muscarinic receptor subtypes where it exhibits low or no efficacy, such as the M5 receptor subtype. A secondary hypothesis is that persistent binding of xanomeline to the M5 receptor results in wash-resistant antagonism to the effects of full agonists. These hypotheses were tested in Chinese hamster ovary cells stably expressing the M5 receptor. In these cells, xanomeline is a weak partial agonist and is able to inhibit carbachol-induced phosphoinositide hydrolysis to the maximal response of xanomeline in a concentration-dependent manner. Pretreatment with xanomeline followed by extensive washing resulted in a significant wash-resistant reduction in receptor affinity with no significant change in maximal cell surface receptor density. This was associated with wash-resistant antagonism of carbachol-induced activation of phosphoinositide hydrolysis at the M5 receptor, reflected as decreased carbachol potency without a change in the maximal response. Similar experiments using the partial agonist pilocarpine demonstrated a reduction of pilocarpine potency as well as maximal response. Our results clearly indicate that wash-resistant binding of xanomeline to the muscarinic M5 receptor is accompanied by persistent antagonism of receptor function. They also suggest a relationship between the efficacy of xanomeline and the functional consequences of its wash-resistant binding at different muscarinic receptor subtypes.