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Drug-Target Interaction

Drug

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PubChem ID:5910
Structure:
Synonyms:
(+)-pilocarpine
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-on
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-one
(3S,4R)-3-ethyl-4-[(3-methylimidazol-4-yl)methyl]oxolan-2-one
(3S,4R)-3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-2(3H)-furanone
(3S-cis)-3-Ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-2(3H)-furanone
(3S-cis)-3-ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone
148-72-1 (NITRATE)
2(3H)-Furanone, 3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-, (3S,4R)-
2(3H)-Furanone, 3-ethyldihydro-4-((1-methyl-1H-imidazol-5-yl)methyl)-, (3S-cis)-
3-Ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-one
54-71-7
54-71-7 (HCL)
91484-73-0
92-13-7
92-13-7 (FREE BASE)
Adsorbocarpine
AI3-50523
AIDS-011876
AIDS011876
Almocarpine
Amistura P
Beta-pilocarpine hydrochloride
BPBio1_000548
BSPBio_000498
BSPBio_002191
C07474
C11H16N2O2
CHEBI:8207
D00525
DB01085
DivK1c_000358
EINECS 202-128-4
Epicar
HSDB 3163
IDI1_000358
Imidazole-5-butyric acid, alpha-ethyl-beta-(hydroxymethyl)-1-methyl-, gamma-lactone
Isopilocarpine
Isoptocarpine
KBio1_000358
KBio2_001587
KBio2_004155
KBio2_006723
KBio3_001691
KBioGR_000956
KBioSS_001587
Lopac0_000950
Lopac0_000960
LS-187208
LS-7661
Mi-Pilo
NCGC00023339-03
NCGC00023339-06
NCGC00023339-07
NCGC00023339-08
NCGC00023339-09
nchembio.78-comp9
NCI60_004403
NINDS_000358
NSC5746 (HCL)
Ocusert
Ocusert P 20
Ocusert pilo
Ocusert pilo-20
Ocusert pilo-20 (TN)
OCUSERT PILO-40
Pilocarpin
Pilocarpine
Pilocarpine (JAN/USP)
Pilocarpine chloride
Pilocarpine HCl
Pilocarpine hydrochloride
Pilocarpine monohydrochloride
Pilocarpine Mononitrate, (3S-cis)-Isomer
Pilocarpine muriate
Pilocarpine nitrate
Pilocarpine nitrate salt
Pilocarpine [USAN:BAN:JAN]
Pilocarpine, Monohydrochloride, (3S-cis)-Isomer
Pilocarpol
Pilokarpin
Pilokarpin monohydrochloride
Pilokarpol
Prestwick0_000449
Prestwick1_000449
Prestwick2_000449
Prestwick3_000449
Salagen
SBB012409
SDCCGMLS-0003164.P005
SPBio_001287
SPBio_002437
Spectrum2_001284
Spectrum3_000546
Spectrum4_000478
Spectrum5_001379
Spectrum_001107
Spersacarpine
Spersacarpine hydrochloride
Syncarpine
Tocris-0694
ZINC00075008
ATC-Codes:

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.