3.5.1.13 (+/-)-huperzine A - 48341 3.5.1.13 1,10-phenanthroline - 62 3.5.1.13 1,10-phenanthroline 20-30% inhibition at 1 mM 62 3.5.1.13 1,2,3,4-tetrahydro-beta-carboline competitive inhibition of AAA-1, slight inhibition of enzyme form AAA-2 31998 3.5.1.13 1,2,3,4-tetrahydro-beta-carboline - 31998 3.5.1.13 1,5-bis(4-allyl-dimethylammonium-phenyl)pentan-3-one-dibromide i.e. BW284c51, inhibition is more pronounced at older developmental stages 83675 3.5.1.13 1-aminohexane - 37988 3.5.1.13 2-bromo-lysergic acid diethylamide marked inhibition of enzyme form AAA1 at pH 7.5, moderate inhibition of enzyme form AAA-1 at pH 5.5 48263 3.5.1.13 2-bromo-lysergic acid diethylamide - 48263 3.5.1.13 2-Hydroxy-5-nitrobenzyl bromide - 3778 3.5.1.13 2-Hydroxy-5-nitrobenzyl bromide inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity 3778 3.5.1.13 2-mercaptoethanol - 63 3.5.1.13 2-mercaptoethanol 52% inhibition at 1 mM 63 3.5.1.13 2-methyl-serotonin - 48526 3.5.1.13 3,4-dichloroaniline - 4204 3.5.1.13 4-chloromercuribenzoate - 388 3.5.1.13 4-chloromercurybenzoate - 206442 3.5.1.13 5-methoxytryptamine slight 8025 3.5.1.13 6-hydroxy-tetrahydroharman slight inhibition of enzyme form AAA-1 and AAA-2 105213 3.5.1.13 8-hydroxyquinoline - 321 3.5.1.13 Acetic anhydride stimulation at low concentrations, inactivation at high concentration 3322 3.5.1.13 Acetic anhydride inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity 3322 3.5.1.13 acetyl-beta-methylcholine bromide - 105353 3.5.1.13 Acetylcholine - 647 3.5.1.13 Acetylcholine serotonin-sensitive aryl acylamidase is inhibited, serotonin-insensitive aryl acylamidase is not inhibited 647 3.5.1.13 acetylcholine iodide - 9422 3.5.1.13 Acetylsalicylic acid - 2261 3.5.1.13 acetylthiocholine iodide - 1086 3.5.1.13 Ag+ 1.0 mM AgNO3, complete inactivation 75 3.5.1.13 Ag+ 0.5 mM AgCl, complete inhibition 75 3.5.1.13 Ag+ 0.1 mM, 6% inhibition 75 3.5.1.13 Ag+ 1.0 mM AgNO3, marked inhibition 75 3.5.1.13 Ag+ complete inhibition at 1 mM 75 3.5.1.13 AgNO3 - 360 3.5.1.13 alpha-methyl-serotonin - 48817 3.5.1.13 benzoylcholine chloride - 96186 3.5.1.13 Bufotenine slight 29825 3.5.1.13 Butyrylcholine iodide - 29833 3.5.1.13 BW284c51 the specific AChE inhibitor inhibits the aryl amidase activity of acetylcholinesterase to a higher extent than the acetylcholinesterase activity 1363 3.5.1.13 BW284c51 - 1363 3.5.1.13 BW284c51 dual site binder, interacts with PAS and the active site of acetylcholinesterase, thus inhibiting both the activities (esterase and aryl acylamidase) 1363 3.5.1.13 Ca2+ inhibits 21.1% at 1 mM and 21.5% at 10 mM 15 3.5.1.13 Carbaryl i.e. 1-naphthyl-N-methylcarbamate, complete inhibition at 0.5 mM 1966 3.5.1.13 catechol 0.5 mM, 73% inhibition 156 3.5.1.13 catechol 0.5 mM, 8.5% inhibition 156 3.5.1.13 Cd2+ complete inhibition at 1 mM 52 3.5.1.13 CdCl2 1.0 mM, complete inactivation 906 3.5.1.13 chlorimipramine enzyme form AAA-1 48203 3.5.1.13 choline chloride - 6500 3.5.1.13 Co2+ inhibits 14.1% at 1 mM and 17.4% at 10 mM 23 3.5.1.13 Co2+ 1 mM: 8.5% activity; strong inhibition 23 3.5.1.13 CoCl2 1.0 mM, 16% inhibition 414 3.5.1.13 Cr2+ - 1919 3.5.1.13 Cu2+ 0.5 mM CuCl2, 86% inhibition 19 3.5.1.13 Cu2+ 0.5 mM CuSO4, 65.5% loss of activity 19 3.5.1.13 Cu2+ 0.1 mM, 9.5% inhibition 19 3.5.1.13 Cu2+ 0.5 mM CuSO4, marked inhibition 19 3.5.1.13 Cu2+ inhibits 13.4% at 1 mM and 45.7% at 10 mM 19 3.5.1.13 Cu2+ 1 mM: 8.9% activity; strong inhibition 19 3.5.1.13 Cu2+ complete inhibition at 1 mM 19 3.5.1.13 CuSO4 - 263 3.5.1.13 cyproheptadine enzyme form AAA-1 7429 3.5.1.13 d-lysergic acid diethylamide marked inhibition of enzyme form AAA1 at pH 7.5, moderate inhibition of enzyme form AAA-1 at pH 5.5 48957 3.5.1.13 d-lysergic acid diethylamide - 48957 3.5.1.13 decamethonium - 21580 3.5.1.13 DFP - 923 3.5.1.13 diethyl dicarbonate - 463 3.5.1.13 diethyl dicarbonate inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity and of aryl acylamidase activity 463 3.5.1.13 diisopropylfluorophosphate complete inhibition of aryl acylacylamidase activity of fatty acid free human albumin at 2 mM, covalent binding to the catalytic site Tyr411 299 3.5.1.13 diisopropylphosphofluoridate complete inhibition at 1 mM , scarcely inhibited at 0.1 mM 3811 3.5.1.13 diisopropylphosphofluoridate - 3811 3.5.1.13 donepezil an Alzheimer drug 2444 3.5.1.13 edrophonium activity is reduced to 64.1% and 30.7% at 0.1 and 0.5 mM. Edrophonium inhibits esterase activity and aryl acylamidase activity of acetylcholinesterase 5271 3.5.1.13 EDTA - 21 3.5.1.13 EDTA 20-30% inhibition at 1 mM 21 3.5.1.13 eserine 0.001 mM, nearly complete inhibition of serum and erythrocyte enzyme, liver enzyme is unaffected 803 3.5.1.13 eserine - 803 3.5.1.13 eserine 0.01 mM, complete, non-competitive 803 3.5.1.13 eserine 97% inhibition of aryl amidase activity at 0.01 mM 803 3.5.1.13 ethopropazine - 2999 3.5.1.13 fasciculin-2 - 33693 3.5.1.13 fatty acid fatty acids block aryl acylamidase activity competing with amides for binding in the catalytic domain 833 3.5.1.13 Fe2+ - 25 3.5.1.13 FeCl3 1.0 mM, 6% inhibition 702 3.5.1.13 formaldehyde - 130 3.5.1.13 harmalol enzyme form of AAA-1 16542 3.5.1.13 harminic acid slight inhibition of enzyme form AAA-1 and AAA-2 106247 3.5.1.13 heptyl-physostigmine - 49106 3.5.1.13 Hg2+ 1 mM: 0% activity; complete inhibition 33 3.5.1.13 Hg2+ complete inhibition at 1 mM 33 3.5.1.13 HgCl2 1.0 mM, complete inactivation 110 3.5.1.13 HgCl2 0.5 mM, 89% inhibition 110 3.5.1.13 HgCl2 - 110 3.5.1.13 HgCl2 0.1 mM, 98% inhibition 110 3.5.1.13 huperzine an Alzheimer drug 17242 3.5.1.13 Indoleamine - 44250 3.5.1.13 iodoacetamide - 67 3.5.1.13 iso-ompa i.e. tetra-isopropyl-pyrophosphoramide, specific inhibitor for BChE, inhibits also the aryl amidase activity 3274 3.5.1.13 iso-ompa inhibitor of butyrylcholinesterase (BChE), also inhibits aryl acylamidase activity 3274 3.5.1.13 malathion 0.06 mM, 75% loss of activity 1888 3.5.1.13 methiothepin enzyme form AAA-1 48204 3.5.1.13 methysergide - 106554 3.5.1.13 Mn2+ - 11 3.5.1.13 additional information phosphatidylinositol-specific phospholipase C of Staphylococcus aureus or sodium deoxycholate-activated endogenous phospholipase C solubilizes serotonin-sensitive arylacylamidase , a loss of activity occurs which can be restored by externally added phosphatidylinositol 2 3.5.1.13 additional information the aryl acylamidase activity is associated with acetylcholinesterase in chicken embryonic brain, and is much more sensitive to Alzheimer drugs, huperzine and donepezil, especially at younger developmental stages, than the esterase activity of the acetylcholinesterase, whereas inhibition of esterase activity is sensitive to tacrine and DFP 2 3.5.1.13 additional information no effect by EDTA, 8-hydroxyquinoline, and 2-mercaptoethanol 2 3.5.1.13 additional information by molecular docking studies the most favourable binding site of aryl acylamidase substrates and serotonin is identified as the side door of acetylcholinesterase. Propidium, a peripheral anionic site binder blocks the main door without affecting the side door, which explains its ineffectiveness in inhibiting aryl acylamidase 2 3.5.1.13 additional information gallamine selectively inhibits the esterase activity to 63.6% (0.1 mM) and 45.4% (0.5 mM), whereas the aryl acylamidase activity remains significantly unaltered in the presence of gallamine (0.1 mM: 105.2%. 0.5 mM: 107%) 2 3.5.1.13 N,N-Dimethyltryptamine slight 12812 3.5.1.13 N-Acetylimidazole stimulation at low concentrations, inactivation at high concentration 1559 3.5.1.13 N-benzyl-N-dodecyl-N,N-dimethylammonium chloride inhibitor at low substrate concentrations 14704 3.5.1.13 N-bromosuccinimide - 208 3.5.1.13 N-methylserotonin - 31927 3.5.1.13 NEM 1.0 mM, 23% inhibition 89 3.5.1.13 NEM - 89 3.5.1.13 neostigmine inhibition of enzyme form AAA-2, no effect of enzyme form AAA-1 2571 3.5.1.13 neostigmine 0.01 mM, nearly complete inhibition of serum and erythrocyte enzyme, liver enzyme is unaffected 2571 3.5.1.13 neostigmine - 2571 3.5.1.13 neostigmine 0.01 mM, complete, non-competitive 2571 3.5.1.13 neostigmine bromide i.e. 1,5-bis(4-allyldimethylammoniumphenyl)pentan-3-one dibromide or BW284C5 7428 3.5.1.13 Ni2+ - 38 3.5.1.13 Ni2+ 0.2 mM NiCl2, 50.2% inhibition 38 3.5.1.13 Ni2+ inhibits 26.0% at 1 mM and 43.2% at 10 mM 38 3.5.1.13 o-Iodosobenzoate 0.25 mM, 27% inhibition 2092 3.5.1.13 p-benzoquinone 0.25 mM, 50% inhibition 2350 3.5.1.13 p-benzoquinone - 2350 3.5.1.13 PCMB 0.25 mM, 61% inhibition 78 3.5.1.13 PCMB - 78 3.5.1.13 physostigmine - 1207 3.5.1.13 PMSF 10 mM: 9.8% activity; strong inhibition 248 3.5.1.13 propionylcholine chloride - 21684 3.5.1.13 puromycin competitive inhibition of hydrolysis L-Ala-4-nitroanilide 657 3.5.1.13 pyridoxal 5'-phosphate inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity 32 3.5.1.13 SDS - 124 3.5.1.13 serotonin - 437 3.5.1.13 serotonin serotonin-sensitive aryl acylamidase, serotonin-insensitive aryl acylamidase is not inhibited 437 3.5.1.13 serotonin non-competitive 437 3.5.1.13 serotonin enzyme from brain is inhibited, liver enzyme is not inhibited; non-competitive 437 3.5.1.13 serotonin 0.5-5 mM, 38-97% inhibition 437 3.5.1.13 serotonin 80% inhibition of aryl amidase activity at 2 mM 437 3.5.1.13 serotonin inhibitor of butyrylcholinesterase (BChE), also inhibits aryl acylamidase activity 437 3.5.1.13 serotonin strong inhibition 437 3.5.1.13 serotonin serotonin inhibits aryl acylamidase while remaining ineffective against the esterase activity. It interacts with D74, N87, L76 and T83 residues of the side door 437 3.5.1.13 serotonin creatinine sulfate - 49415 3.5.1.13 serotonin creatinine sulfate moderate inhibition of enzyme form AAA-1 at pH 7.5, no inhibition of enzyme form AAA-2 at pH 5.5 49415 3.5.1.13 Sodium arsenate - 3229 3.5.1.13 Sodium thioglycolate - 4566 3.5.1.13 Succinylcholine chloride - 44844 3.5.1.13 tacrine - 1456 3.5.1.13 tetrahydroharman - 107344 3.5.1.13 tetraisopropyldiphosphoramide weak 11159 3.5.1.13 tetraisopropyldiphosphoramide - 11159 3.5.1.13 Tetranitromethane stimulation at low concentrations, inactivation at high concentration 1453 3.5.1.13 Trinitrobenzenesulfonic acid - 6605 3.5.1.13 Trinitrobenzenesulfonic acid inactivates aryl acylamidase activity and acetylcholinesterase activity in absence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one. Presence of acetylcholine or 1,5-bis[4-(allyl-dimethylammonium)phenyl]pentan-3-one prevents loss of acetylcholinesterase activity but not of aryl acylamidase activity 6605 3.5.1.13 Triton X-100 - 61 3.5.1.13 tryptamine slight inhibition of enzyme form AAA-1 at pH 7.5, no inhibition of enzyme form AAA-2 at pH 5.5 363 3.5.1.13 tryptamine - 363 3.5.1.13 tryptamine hydrochloride - 107449 3.5.1.13 Tween-80 - 2672 3.5.1.13 tyramine inhibitor of hydrolysis for charged substrates 280 3.5.1.13 Urea 6 M, irreversible inactivation 116 3.5.1.13 Zn2+ - 14 3.5.1.13 Zn2+ 0.1 mM, 51% inhibition 14 3.5.1.13 Zn2+ inhibits 40.0% at 1 mM and 75.8% at 10 mM 14