Proteins > Muscarinic acetylcholine receptor M2
Page last updated: 2024-08-07 15:45:24
Muscarinic acetylcholine receptor M2
A muscarinic acetylcholine receptor M2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P08172]
Synonyms
Research
Bioassay Publications (143)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 9 (6.29) | 18.7374 |
| 1990's | 30 (20.98) | 18.2507 |
| 2000's | 46 (32.17) | 29.6817 |
| 2010's | 48 (33.57) | 24.3611 |
| 2020's | 10 (6.99) | 2.80 |
Compounds (182)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| quinacrine | Homo sapiens (human) | IC50 | 0.9640 | 1 | 0 |
| quinacrine | Homo sapiens (human) | Ki | 0.3430 | 1 | 0 |
| tacrine | Homo sapiens (human) | Ki | 5.8000 | 1 | 1 |
| methacholine | Homo sapiens (human) | IC50 | 2.7900 | 2 | 2 |
| methacholine | Homo sapiens (human) | Ki | 0.0590 | 1 | 1 |
| amiodarone | Homo sapiens (human) | IC50 | 5.0800 | 1 | 0 |
| amiodarone | Homo sapiens (human) | Ki | 1.8060 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | IC50 | 0.0810 | 1 | 0 |
| amitriptyline | Homo sapiens (human) | Ki | 0.0290 | 1 | 0 |
| amoxapine | Homo sapiens (human) | IC50 | 2.6230 | 1 | 0 |
| amoxapine | Homo sapiens (human) | Ki | 0.9330 | 1 | 0 |
| 1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid prop-2-ynyl ester | Homo sapiens (human) | Ki | 0.5322 | 2 | 2 |
| arecoline | Homo sapiens (human) | IC50 | 3.6000 | 2 | 3 |
| arecoline | Homo sapiens (human) | Ki | 0.9949 | 5 | 5 |
| astemizole | Homo sapiens (human) | IC50 | 1.4090 | 1 | 0 |
| astemizole | Homo sapiens (human) | Ki | 0.5010 | 1 | 0 |
| bethanechol | Homo sapiens (human) | Ki | 0.0970 | 1 | 1 |
| biperiden | Homo sapiens (human) | Ki | 0.0137 | 1 | 1 |
| carbamylcholine | Homo sapiens (human) | Ki | 0.0050 | 1 | 1 |
| carbetapentane | Homo sapiens (human) | Ki | 0.1670 | 1 | 1 |
| chloroquine | Homo sapiens (human) | Ki | 4.6774 | 1 | 1 |
| chlorpromazine | Homo sapiens (human) | IC50 | 0.6520 | 1 | 0 |
| chlorpromazine | Homo sapiens (human) | Ki | 0.2320 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | IC50 | 21.1070 | 1 | 0 |
| ciglitazone | Homo sapiens (human) | Ki | 7.5050 | 1 | 0 |
| clomipramine | Homo sapiens (human) | IC50 | 0.2410 | 1 | 0 |
| clomipramine | Homo sapiens (human) | Ki | 0.0860 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | IC50 | 14.5310 | 1 | 0 |
| clotrimazole | Homo sapiens (human) | Ki | 5.1670 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | IC50 | 0.0350 | 1 | 0 |
| cyproheptadine | Homo sapiens (human) | Ki | 0.0080 | 2 | 1 |
| dicyclomine | Homo sapiens (human) | IC50 | 0.0460 | 1 | 0 |
| dicyclomine | Homo sapiens (human) | Ki | 0.0160 | 1 | 0 |
| diphenidol | Homo sapiens (human) | IC50 | 0.7700 | 1 | 0 |
| diphenidol | Homo sapiens (human) | Ki | 0.2740 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | IC50 | 1.0500 | 1 | 0 |
| diphenhydramine | Homo sapiens (human) | Ki | 0.3730 | 1 | 0 |
| doxepin | Homo sapiens (human) | IC50 | 0.2580 | 1 | 0 |
| doxepin | Homo sapiens (human) | Ki | 0.0920 | 1 | 0 |
| ebastine | Homo sapiens (human) | IC50 | 0.8930 | 2 | 1 |
| ebastine | Homo sapiens (human) | Ki | 0.2795 | 1 | 0 |
| econazole | Homo sapiens (human) | IC50 | 3.2560 | 1 | 0 |
| econazole | Homo sapiens (human) | Ki | 1.1580 | 1 | 0 |
| eperisone | Homo sapiens (human) | IC50 | 2.3380 | 1 | 0 |
| eperisone | Homo sapiens (human) | Ki | 0.8310 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | IC50 | 7.4810 | 1 | 0 |
| fluphenazine | Homo sapiens (human) | Ki | 2.6600 | 1 | 0 |
| 2-cyclopentyl-2-hydroxy-2-phenylacetic acid (1,1-dimethyl-3-pyrrolidin-1-iumyl) ester | Homo sapiens (human) | IC50 | 0.0002 | 1 | 1 |
| haloperidol | Homo sapiens (human) | Ki | 4.6700 | 1 | 1 |
| hydroxychloroquine | Homo sapiens (human) | IC50 | 2.9510 | 1 | 0 |
| hydroxychloroquine | Homo sapiens (human) | Ki | 3.0888 | 2 | 1 |
| ketoconazole | Homo sapiens (human) | IC50 | 26.3460 | 1 | 0 |
| ketoconazole | Homo sapiens (human) | Ki | 9.3680 | 1 | 0 |
| ketotifen | Homo sapiens (human) | IC50 | 0.8380 | 1 | 0 |
| ketotifen | Homo sapiens (human) | Ki | 0.2980 | 1 | 0 |
| maprotiline | Homo sapiens (human) | IC50 | 1.9270 | 1 | 0 |
| maprotiline | Homo sapiens (human) | Ki | 0.6850 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | IC50 | 1.6650 | 1 | 0 |
| methapyrilene | Homo sapiens (human) | Ki | 0.5920 | 1 | 0 |
| methoctramine | Homo sapiens (human) | IC50 | 0.0407 | 3 | 3 |
| methoctramine | Homo sapiens (human) | Ki | 0.0211 | 5 | 5 |
| n-methylcarbamylcholine | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
| 5-methylfurtrethonium | Homo sapiens (human) | Ki | 0.9550 | 1 | 1 |
| mianserin | Homo sapiens (human) | IC50 | 1.0780 | 1 | 0 |
| mianserin | Homo sapiens (human) | Ki | 0.3830 | 1 | 0 |
| miconazole | Homo sapiens (human) | IC50 | 4.3360 | 1 | 0 |
| miconazole | Homo sapiens (human) | Ki | 1.5420 | 1 | 0 |
| mitoxantrone | Homo sapiens (human) | IC50 | 0.2190 | 1 | 0 |
| mitoxantrone | Homo sapiens (human) | Ki | 0.0779 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | IC50 | 0.3470 | 1 | 0 |
| nortriptyline | Homo sapiens (human) | Ki | 0.1230 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | IC50 | 0.3760 | 1 | 0 |
| orphenadrine | Homo sapiens (human) | Ki | 0.1340 | 1 | 0 |
| oxotremorine | Homo sapiens (human) | IC50 | 0.4000 | 1 | 2 |
| oxotremorine | Homo sapiens (human) | Ki | 2.7557 | 9 | 9 |
| oxybutynin | Homo sapiens (human) | IC50 | 0.0270 | 1 | 0 |
| oxybutynin | Homo sapiens (human) | Ki | 0.0114 | 4 | 3 |
| pentamidine | Homo sapiens (human) | IC50 | 1.4250 | 1 | 0 |
| pentamidine | Homo sapiens (human) | Ki | 0.5070 | 1 | 0 |
| pirenzepine | Homo sapiens (human) | IC50 | 0.6891 | 2 | 2 |
| pirenzepine | Homo sapiens (human) | Ki | 0.3744 | 4 | 4 |
| prochlorperazine | Homo sapiens (human) | IC50 | 3.1120 | 1 | 0 |
| prochlorperazine | Homo sapiens (human) | Ki | 1.1070 | 1 | 0 |
| promazine | Homo sapiens (human) | IC50 | 1.0890 | 1 | 0 |
| promazine | Homo sapiens (human) | Ki | 0.3870 | 1 | 0 |
| promethazine | Homo sapiens (human) | IC50 | 0.0350 | 1 | 0 |
| promethazine | Homo sapiens (human) | Ki | 0.0120 | 1 | 0 |
| propranolol | Homo sapiens (human) | IC50 | 5.0119 | 1 | 1 |
| pyridostigmine | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| quetiapine | Homo sapiens (human) | IC50 | 3.3447 | 1 | 0 |
| quetiapine | Homo sapiens (human) | Ki | 1.1046 | 2 | 1 |
| risperidone | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| sdz 205-557 | Homo sapiens (human) | IC50 | 0.2512 | 1 | 1 |
| spiperone | Homo sapiens (human) | Ki | 49.6000 | 1 | 1 |
| thioridazine | Homo sapiens (human) | IC50 | 0.1060 | 1 | 0 |
| thioridazine | Homo sapiens (human) | Ki | 0.0380 | 1 | 0 |
| trihexyphenidyl | Homo sapiens (human) | IC50 | 0.0340 | 1 | 0 |
| trihexyphenidyl | Homo sapiens (human) | Ki | 0.0120 | 1 | 0 |
| tropicamide | Homo sapiens (human) | IC50 | 0.1050 | 1 | 0 |
| tropicamide | Homo sapiens (human) | Ki | 0.0370 | 1 | 0 |
| carbachol | Homo sapiens (human) | IC50 | 17.6728 | 7 | 7 |
| carbachol | Homo sapiens (human) | Ki | 1.2977 | 15 | 15 |
| pilocarpine | Homo sapiens (human) | Ki | 12.0226 | 1 | 1 |
| (4-(m-chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium chloride | Homo sapiens (human) | Ki | 3.2359 | 2 | 2 |
| mepazine | Homo sapiens (human) | IC50 | 0.5650 | 1 | 0 |
| mepazine | Homo sapiens (human) | Ki | 0.2010 | 1 | 0 |
| gallamine triethiodide | Homo sapiens (human) | IC50 | 1.3876 | 2 | 1 |
| gallamine triethiodide | Homo sapiens (human) | Ki | 1.6314 | 3 | 2 |
| mepenzolate bromide | Homo sapiens (human) | Ki | 0.0014 | 2 | 2 |
| cyclizine | Homo sapiens (human) | IC50 | 1.1580 | 1 | 0 |
| cyclizine | Homo sapiens (human) | Ki | 0.4120 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | IC50 | 0.5740 | 1 | 0 |
| benzethonium chloride | Homo sapiens (human) | Ki | 0.2040 | 1 | 0 |
| sterogenol | Homo sapiens (human) | IC50 | 0.1160 | 1 | 0 |
| sterogenol | Homo sapiens (human) | Ki | 0.0410 | 1 | 0 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| muscarine | Homo sapiens (human) | IC50 | 2.1745 | 2 | 2 |
| muscarine | Homo sapiens (human) | Ki | 0.1654 | 4 | 4 |
| dimenhydrinate | Homo sapiens (human) | IC50 | 0.4610 | 1 | 0 |
| dimenhydrinate | Homo sapiens (human) | Ki | 0.1640 | 1 | 0 |
| gentian violet | Homo sapiens (human) | IC50 | 1.4300 | 1 | 0 |
| gentian violet | Homo sapiens (human) | Ki | 0.5080 | 1 | 0 |
| glycopyrrolate | Homo sapiens (human) | IC50 | 0.0005 | 1 | 1 |
| glycopyrrolate | Homo sapiens (human) | Ki | 0.0016 | 1 | 1 |
| ethylestrenol | Homo sapiens (human) | IC50 | 0.2920 | 1 | 0 |
| ethylestrenol | Homo sapiens (human) | Ki | 0.1040 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | IC50 | 12.4660 | 1 | 0 |
| 4-octylphenol | Homo sapiens (human) | Ki | 4.4320 | 1 | 0 |
| benzetimide | Homo sapiens (human) | IC50 | 5.0005 | 1 | 2 |
| dimethindene | Homo sapiens (human) | Ki | 0.0447 | 1 | 1 |
| quinuclidinyl benzilate | Homo sapiens (human) | Ki | 0.0001 | 5 | 7 |
| clemastine | Homo sapiens (human) | Ki | 0.1175 | 1 | 1 |
| dexchlorpheniramine | Homo sapiens (human) | IC50 | 6.9940 | 1 | 0 |
| dexchlorpheniramine | Homo sapiens (human) | Ki | 2.4870 | 1 | 0 |
| butaclamol | Homo sapiens (human) | Ki | 5.2000 | 1 | 1 |
| paroxetine | Homo sapiens (human) | IC50 | 0.5320 | 1 | 0 |
| paroxetine | Homo sapiens (human) | Ki | 0.1890 | 1 | 0 |
| n-methyl-n-(1-methyl-4-pyrrolidino-2-butynyl)acetamide | Homo sapiens (human) | Ki | 0.3300 | 1 | 1 |
| sertindole | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| xanomeline | Homo sapiens (human) | IC50 | 0.1644 | 2 | 2 |
| xanomeline | Homo sapiens (human) | Ki | 0.5456 | 13 | 13 |
| ziprasidone | Homo sapiens (human) | Ki | 5.0000 | 1 | 1 |
| trihexyphenidyl hydrochloride | Homo sapiens (human) | IC50 | 0.0186 | 1 | 1 |
| diphenidol hydrochloride | Homo sapiens (human) | Ki | 2.8184 | 1 | 1 |
| sertraline | Homo sapiens (human) | IC50 | 2.7675 | 1 | 0 |
| sertraline | Homo sapiens (human) | Ki | 0.9840 | 1 | 0 |
| esaprazole | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| aprofen | Homo sapiens (human) | Ki | 0.0476 | 4 | 4 |
| n-methylscopolamine | Homo sapiens (human) | IC50 | 0.3350 | 4 | 4 |
| n-methylscopolamine | Homo sapiens (human) | Ki | 0.0012 | 14 | 14 |
| methoctramine | Homo sapiens (human) | IC50 | 0.0315 | 2 | 2 |
| methoctramine | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| gr 127935 | Homo sapiens (human) | Ki | 3.2500 | 4 | 4 |
| afdx 116 | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
| afdx 116 | Homo sapiens (human) | Ki | 0.0810 | 1 | 1 |
| afdx 384 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| pramipexole | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sb 204070a | Homo sapiens (human) | IC50 | 0.0001 | 1 | 1 |
| desloratadine | Homo sapiens (human) | IC50 | 0.1070 | 1 | 0 |
| desloratadine | Homo sapiens (human) | Ki | 0.0380 | 1 | 0 |
| l 670548 | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| azaprophen | Homo sapiens (human) | Ki | 0.0004 | 2 | 2 |
| aq-ra 741 | Homo sapiens (human) | Ki | 0.0046 | 2 | 2 |
| bibn 99 | Homo sapiens (human) | Ki | 0.0302 | 1 | 1 |
| tripitramine | Homo sapiens (human) | Ki | 0.0003 | 2 | 2 |
| solifenacin | Homo sapiens (human) | Ki | 0.1202 | 1 | 1 |
| hyoscyamine | Homo sapiens (human) | Ki | 0.0058 | 5 | 5 |
| harmalan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| hexamethylenebis(dimethyl-(3-phthalimidopropyl)ammonium bromide) | Homo sapiens (human) | IC50 | 0.4786 | 1 | 1 |
| hexamethylenebis(dimethyl-(3-phthalimidopropyl)ammonium bromide) | Homo sapiens (human) | Ki | 0.5614 | 8 | 8 |
| atropine | Homo sapiens (human) | IC50 | 0.0067 | 3 | 2 |
| atropine | Homo sapiens (human) | Ki | 0.0038 | 21 | 22 |
| nantenine, (+-)-isomer | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| solifenacin succinate | Homo sapiens (human) | IC50 | 0.5737 | 1 | 1 |
| 5-((4-(4-(diethylamino)butyl)-1-piperidinyl)acetyl)-10,11-dihydrobenzo(b,e)(1,4)diazepine-11-one | Homo sapiens (human) | Ki | 0.0003 | 1 | 1 |
| 1-methyl-6-methoxy-dihydro-beta-carboline | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| terconazole | Homo sapiens (human) | IC50 | 12.9090 | 1 | 0 |
| terconazole | Homo sapiens (human) | Ki | 4.5900 | 1 | 0 |
| tolterodine | Homo sapiens (human) | Ki | 0.0034 | 2 | 2 |
| darifenacin | Homo sapiens (human) | Ki | 0.0363 | 3 | 3 |
| tropisetron | Homo sapiens (human) | IC50 | 3.1623 | 1 | 1 |
| ipratropium bromide anhydrous | Homo sapiens (human) | IC50 | 0.0021 | 2 | 2 |
| ipratropium bromide anhydrous | Homo sapiens (human) | Ki | 0.0008 | 4 | 4 |
| ipratropium | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
| methamilane methiodide | Homo sapiens (human) | Ki | 1.2023 | 1 | 1 |
| quinuclidinyl benzilate | Homo sapiens (human) | IC50 | 0.0004 | 1 | 1 |
| 4,4-dicarboxy-5-pyridoxylproline | Homo sapiens (human) | Ki | 19.9526 | 1 | 1 |
| benztropine | Homo sapiens (human) | IC50 | 0.0366 | 2 | 1 |
| benztropine | Homo sapiens (human) | Ki | 0.0037 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | IC50 | 3.6280 | 1 | 0 |
| enclomiphene | Homo sapiens (human) | Ki | 1.2900 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | IC50 | 7.7930 | 1 | 0 |
| tamoxifen | Homo sapiens (human) | Ki | 2.7710 | 1 | 0 |
| vicriviroc | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | IC50 | 0.0550 | 1 | 1 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | Ki | 0.0230 | 1 | 1 |
| 4-[[(4-methylphenyl)sulfonylamino]methyl]-N-[2-[(phenylmethyl)-propan-2-ylamino]ethyl]benzamide | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| sb-224289 | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| harmine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| trospium chloride | Homo sapiens (human) | Ki | 0.0011 | 1 | 1 |
| cp 481715 | Homo sapiens (human) | Ki | 1.3230 | 1 | 1 |
| l 745870 | Homo sapiens (human) | Ki | 10.0000 | 2 | 2 |
| tiotropium bromide | Homo sapiens (human) | Ki | 0.0005 | 1 | 1 |
| tiotropium | Homo sapiens (human) | Ki | 0.0002 | 1 | 1 |
| homatropine hydrobromide, (endo-(+-)-isomer) | Homo sapiens (human) | IC50 | 0.2120 | 1 | 0 |
| homatropine hydrobromide, (endo-(+-)-isomer) | Homo sapiens (human) | Ki | 0.0750 | 1 | 0 |
| himbacine | Homo sapiens (human) | IC50 | 0.0175 | 1 | 1 |
| himbacine | Homo sapiens (human) | Ki | 0.0234 | 5 | 6 |
| fm1 43 | Homo sapiens (human) | Ki | 0.0550 | 1 | 1 |
| milameline | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| sabcomeline | Homo sapiens (human) | IC50 | 0.1800 | 1 | 1 |
| sabcomeline | Homo sapiens (human) | Ki | 0.2042 | 1 | 1 |
| pd 144418 | Homo sapiens (human) | Ki | 23.9883 | 1 | 1 |
| ac 260584 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| 4-n-butyl-1-(4-(2-methylphenyl)-4-oxo-1-butyl)-piperidine hydrogen chloride | Homo sapiens (human) | Ki | 0.9900 | 2 | 2 |
| tert-butyl peroxybenzoate | Homo sapiens (human) | IC50 | 3.4837 | 1 | 2 |
| tert-butyl peroxybenzoate | Homo sapiens (human) | Ki | 0.3200 | 1 | 1 |
| 77-lh-28-1 | Homo sapiens (human) | Ki | 0.2042 | 1 | 1 |
| PB28 | Homo sapiens (human) | Ki | 4.7863 | 1 | 1 |
| amd 070 | Homo sapiens (human) | IC50 | 12.2500 | 2 | 2 |
| naluzotan | Homo sapiens (human) | Ki | 2.0000 | 1 | 1 |
| tiotropium bromide | Homo sapiens (human) | IC50 | 0.0001 | 4 | 4 |
| tiotropium bromide | Homo sapiens (human) | Ki | 0.0001 | 5 | 5 |
| aclidinium bromide | Homo sapiens (human) | IC50 | 0.0001 | 3 | 3 |
| aclidinium bromide | Homo sapiens (human) | Ki | 0.0003 | 2 | 2 |
| bencycloquidium bromide | Homo sapiens (human) | Ki | 0.0062 | 1 | 1 |
| ly2033298 | Homo sapiens (human) | Ki | 1.6604 | 2 | 2 |
| td-4208 | Homo sapiens (human) | Ki | 0.0050 | 2 | 0 |
| scopolamine hydrobromide | Homo sapiens (human) | Ki | 0.0086 | 6 | 6 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| sp 203 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| srt1720 | Homo sapiens (human) | IC50 | 6.2800 | 1 | 1 |
| cep 26401 | Homo sapiens (human) | Ki | 3.7000 | 1 | 1 |
| azd7687 | Homo sapiens (human) | IC50 | 80.5000 | 1 | 1 |
| nitd 609 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| tetracycline | Homo sapiens (human) | IC50 | 140.0000 | 1 | 1 |
| entecavir | Homo sapiens (human) | Ki | 0.0720 | 1 | 0 |
| clozapine | Homo sapiens (human) | IC50 | 0.4760 | 1 | 0 |
| clozapine | Homo sapiens (human) | Ki | 0.1015 | 2 | 1 |
| olanzapine | Homo sapiens (human) | Ki | 0.0260 | 1 | 1 |
| norclozapine | Homo sapiens (human) | Ki | 0.2500 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| nifedipine | Homo sapiens (human) | ID50 | 700,000.0050 | 2 | 2 |
| oxybutynin | Homo sapiens (human) | Kb | 0.0980 | 1 | 4 |
| carbachol | Homo sapiens (human) | ED50 | 0.2700 | 1 | 1 |
| uridine triphosphate | Homo sapiens (human) | Km | 15.0000 | 1 | 1 |
| metergoline | Homo sapiens (human) | Activity | 0.0177 | 1 | 1 |
| 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester | Homo sapiens (human) | ID50 | 4,000,000.0000 | 1 | 1 |
| oxybutynin hydrochloride | Homo sapiens (human) | Kb | 0.0050 | 1 | 1 |
| 1,4-dihydro-2,6-dimethyl-4-(4-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl ester | Homo sapiens (human) | ID50 | 3,200,000.0000 | 1 | 1 |
| atropine | Homo sapiens (human) | ED50 | 0.0001 | 2 | 2 |
| atropine | Homo sapiens (human) | ID50 | 0.0001 | 1 | 1 |
| atropine | Homo sapiens (human) | Kb | 0.0015 | 2 | 5 |
| 4-diphenylacetoxy-n-methylpiperidine methiodide | Homo sapiens (human) | Kb | 0.0085 | 1 | 1 |
| imidafenacin | Homo sapiens (human) | Kb | 0.0041 | 2 | 2 |
| caproctamine | Homo sapiens (human) | Kb | 0.4100 | 1 | 1 |
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 8, Issue:20, 1998
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.Journal of medicinal chemistry, , Jan-01, Volume: 41, Issue:1, 1998
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.Journal of medicinal chemistry, , Jun-12, Volume: 57, Issue:11, 2014
Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.European journal of medicinal chemistry, , Volume: 63, 2013
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties.Bioorganic & medicinal chemistry, , Mar-15, Volume: 15, Issue:6, 2007
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.Journal of medicinal chemistry, , Nov-03, Volume: 48, Issue:22, 2005
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Structure-activity relationships among methoctramine-related polymethylene tetraamines. Chain-length and substituent effects on M-2 muscarinic receptor blocking activity.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Synthesis and calcium channel antagonist activity of dialkyl 4- (dihydropyridinyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylates.Journal of medicinal chemistry, , Volume: 30, Issue:4, 1987
Synthesis and calcium channel antagonist activity of dialkyl 1,4-dihydro-2,6-dimethyl-4-(pyridinyl)-3,5-pyridinedicarboxylates.Journal of medicinal chemistry, , Volume: 29, Issue:12, 1986
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Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity.Journal of medicinal chemistry, , Jan-01, Volume: 41, Issue:1, 1998
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones.Journal of medicinal chemistry, , Volume: 33, Issue:2, 1990
1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 17, Issue:4, 2007
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Synthesis and antimuscarinic properties of some N-substituted 5-(aminomethyl)-3,3-diphenyl-2(3H)-furanones.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
[no title available],
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Identification and characterization of m1 selective muscarinic receptor antagonists1.Journal of medicinal chemistry, , Feb-11, Volume: 42, Issue:3, 1999
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.Journal of medicinal chemistry, , Volume: 32, Issue:6, 1989
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
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Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 17, Issue:24, 2009
Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists.Journal of medicinal chemistry, , Jul-10, Volume: 51, Issue:13, 2008
Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists.Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Highly chiral muscarinic ligands: the discovery of (2S,2'R,3'S,5'R)-1-methyl-2-(2-methyl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide methyl iodide, a potent, functionally selective, M2 partial agonist.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the bindJournal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 8, Issue:20, 1998
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist.Journal of medicinal chemistry, , Jul-02, Volume: 41, Issue:14, 1998
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.Journal of medicinal chemistry, , Jun-09, Volume: 38, Issue:12, 1995
Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine.Journal of medicinal chemistry, , Volume: 31, Issue:1, 1988
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 8, Issue:20, 1998
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation.Bioorganic & medicinal chemistry, , Dec-15, Volume: 17, Issue:24, 2009
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.Bioorganic & medicinal chemistry, , Jul-01, Volume: 22, Issue:13, 2014
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.Journal of medicinal chemistry, , Jun-04, Volume: 41, Issue:12, 1998
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
The discovery of new spirocyclic muscarinic M3 antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.Journal of medicinal chemistry, , Nov-07, Volume: 40, Issue:23, 1997
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.Journal of medicinal chemistry, , Feb-03, Volume: 38, Issue:3, 1995
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine MJournal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the MJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M₁ agonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the bindJournal of medicinal chemistry, , Dec-14, Volume: 49, Issue:25, 2006
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders.Journal of medicinal chemistry, , Sep-25, Volume: 46, Issue:20, 2003
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives.Journal of medicinal chemistry, , Jun-03, Volume: 42, Issue:11, 1999
Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.Bioorganic & medicinal chemistry, , May-01, Volume: 21, Issue:9, 2013
Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues).Journal of medicinal chemistry, , Apr-03, Volume: 35, Issue:7, 1992
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.Journal of medicinal chemistry, , Volume: 30, Issue:5, 1987
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine MJournal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the MJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.Journal of medicinal chemistry, , Feb-23, Volume: 55, Issue:4, 2012
Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure.Journal of medicinal chemistry, , Mar-22, Volume: 50, Issue:6, 2007
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.Journal of medicinal chemistry, , Jul-24, Volume: 51, Issue:14, 2008
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
Differential blockade of muscarinic receptor subtypes by polymethylene tetraamines. Novel class of selective antagonists of cardiac M-2 muscarinic receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Evolution of a novel series of [(N,N-dimethylamino)propyl]- and piperazinylbenzanilides as the first selective 5-HT1D antagonists.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane.Journal of medicinal chemistry, , Mar-06, Volume: 35, Issue:5, 1992
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
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Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine MJournal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the MJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine MJournal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human MBioorganic & medicinal chemistry letters, , 02-01, Volume: 29, Issue:3, 2019
Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the MJournal of medicinal chemistry, , 04-27, Volume: 60, Issue:8, 2017
Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.Bioorganic & medicinal chemistry, , May-01, Volume: 21, Issue:9, 2013
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Pyridophens: binary pyridostigmine-aprophen prodrugs with differential inhibition of acetylcholinesterase, butyrylcholinesterase, and muscarinic receptors.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships.Journal of medicinal chemistry, , Nov-07, Volume: 40, Issue:23, 1997
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands.Journal of medicinal chemistry, , Jul-22, Volume: 37, Issue:15, 1994
Synthesis and antimuscarinic activity of some 1-cycloalkyl-1-hydroxy-1-phenyl-3-(4-substituted piperazinyl)-2-propanones and related compounds.Journal of medicinal chemistry, , Mar-05, Volume: 36, Issue:5, 1993
Synthesis and antimuscarinic properties of some N-substituted 5-(aminomethyl)-3,3-diphenyl-2(3H)-furanones.Journal of medicinal chemistry, , Nov-13, Volume: 35, Issue:23, 1992
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen.Journal of medicinal chemistry, , Volume: 34, Issue:4, 1991
Structure-activity relationships among methoctramine-related polymethylene tetraamines. Chain-length and substituent effects on M-2 muscarinic receptor blocking activity.Journal of medicinal chemistry, , Volume: 32, Issue:1, 1989
Enantioselectivity of muscarinic antagonists. 2,2-Dicyclohexyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodides and related 3-oxides.Journal of medicinal chemistry, , Volume: 31, Issue:9, 1988
Differential blockade of muscarinic receptor subtypes by polymethylene tetraamines. Novel class of selective antagonists of cardiac M-2 muscarinic receptors.Journal of medicinal chemistry, , Volume: 30, Issue:1, 1987
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.Journal of medicinal chemistry, , Volume: 30, Issue:5, 1987
[no title available],
Design and synthesis of a fluorescent muscarinic antagonist.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Regiospecific Introduction of Halogens on the 2-Aminobiphenyl Subunit Leading to Highly Potent and Selective M3 Muscarinic Acetylcholine Receptor Antagonists and Weak Inverse Agonists.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 16, Issue:2, 2006
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes.Journal of medicinal chemistry, , Feb-14, Volume: 45, Issue:4, 2002
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 25, Issue:8, 2015
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)aceJournal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
Discovery of MJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Design, synthesis and antimuscarinic activity of some imidazolium derivatives.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function bJournal of medicinal chemistry, , Apr-09, Volume: 41, Issue:8, 1998
Discovery of MJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Design, synthesis and antimuscarinic activity of some imidazolium derivatives.Bioorganic & medicinal chemistry letters, , Oct-18, Volume: 9, Issue:20, 1999
Novel imidazole derivatives with subtype-selective antimuscarinic activity (1).Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.Bioorganic & medicinal chemistry letters, , Aug-02, Volume: 14, Issue:15, 2004
Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists.Bioorganic & medicinal chemistry letters, , Aug-05, Volume: 12, Issue:15, 2002
Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine.Bioorganic & medicinal chemistry letters, , Oct-21, Volume: 12, Issue:20, 2002
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.Bioorganic & medicinal chemistry letters, , May-07, Volume: 11, Issue:9, 2001
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-22, Volume: 9, Issue:6, 1999
Identification and characterization of m4 selective muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M₁ agonists.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 25, Issue:19, 2015
Docking analyses on human muscarinic receptors: unveiling the subtypes peculiarities in agonists binding.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.Journal of medicinal chemistry, , Dec-19, Volume: 40, Issue:26, 1997
Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Multi-target-directed ligands to combat neurodegenerative diseases.Journal of medicinal chemistry, , Feb-14, Volume: 51, Issue:3, 2008
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 23, Issue:1, 2013
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 18, Issue:20, 2008
[no title available]Journal of medicinal chemistry, , 03-10, Volume: 65, Issue:5, 2022
Discovery of ACS medicinal chemistry letters, , May-10, Volume: 9, Issue:5, 2018
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 25, Issue:8, 2015
Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
The discovery of AZD9164, a novel muscarinic M3 antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 21, Issue:24, 2011
Inhalation by design: novel tertiary amine muscarinic M₃ receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease.Journal of medicinal chemistry, , Oct-13, Volume: 54, Issue:19, 2011
The discovery of new spirocyclic muscarinic M3 antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)aceJournal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 18, Issue:8, 2008
Chemical modification-mediated optimisation of bronchodilatory activity of mepenzolate, a muscarinic receptor antagonist with anti-inflammatory activity.Bioorganic & medicinal chemistry, , 08-01, Volume: 27, Issue:15, 2019
The discovery of AZD9164, a novel muscarinic M3 antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 21, Issue:24, 2011
The discovery of new spirocyclic muscarinic M3 antagonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)aceJournal of medicinal chemistry, , Aug-27, Volume: 52, Issue:16, 2009
Dualsteric muscarinic antagonists--orthosteric binding pose controls allosteric subtype selectivity.Journal of medicinal chemistry, , Aug-14, Volume: 57, Issue:15, 2014
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.Journal of medicinal chemistry, , Feb-28, Volume: 56, Issue:4, 2013
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Selective optimization of side activities: another way for drug discovery.Journal of medicinal chemistry, , Mar-11, Volume: 47, Issue:6, 2004
[no title available],
Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors.Bioorganic & medicinal chemistry letters, , 05-15, Volume: 40, 2021
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled acetylcholine receptor activity | molecular function | Combining with acetylcholine and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, GOC:fj, GOC:mah] |
| arrestin family protein binding | molecular function | Binding to a member of the arrestin family, proteins involved in agonist-mediated desensitization of G protein-coupled receptors. [PMID:23911909] |
| G protein-coupled serotonin receptor activity | molecular function | Combining with the biogenic amine serotonin and transmitting the signal across the membrane by activating an associated G-protein. Serotonin (5-hydroxytryptamine) is a neurotransmitter and hormone found in vertebrates and invertebrates. [GOC:ai] |
Located In
This protein is located in 11 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| clathrin-coated endocytic vesicle membrane | cellular component | The lipid bilayer surrounding a clathrin-coated endocytic vesicle. [GOC:mah] |
| asymmetric synapse | cellular component | A type of synapse occurring between an axon and a dendritic spine or dendritic shaft. Asymmetric synapses, the most abundant synapse type in the central nervous system, involve axons that contain predominantly spherical vesicles and contain a thickened postsynaptic density. Most or all synapses of this type are excitatory. [GOC:dgh, GOC:ef] |
| symmetric synapse | cellular component | A synapse that lacks an electron dense postsynaptic specialization. In vertebtrates, these occur primarily on dendrite shafts and neuronal cell bodies and involve persynapses containing clusters of predominantly flattened or elongated vesicles and are typcially inhibitory. [GOC:dgh, GOC:ef] |
| presynaptic membrane | cellular component | A specialized area of membrane of the axon terminal that faces the plasma membrane of the neuron or muscle fiber with which the axon terminal establishes a synaptic junction; many synaptic junctions exhibit structural presynaptic characteristics, such as conical, electron-dense internal protrusions, that distinguish it from the remainder of the axon plasma membrane. [GOC:jl, ISBN:0815316194] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
| axon terminus | cellular component | Terminal inflated portion of the axon, containing the specialized apparatus necessary to release neurotransmitters. The axon terminus is considered to be the whole region of thickening and the terminal button is a specialized region of it. [GOC:dph, GOC:jl] |
| postsynaptic membrane | cellular component | A specialized area of membrane facing the presynaptic membrane on the tip of the nerve ending and separated from it by a minute cleft (the synaptic cleft). Neurotransmitters cross the synaptic cleft and transmit the signal to the postsynaptic membrane. [ISBN:0198506732] |
| glutamatergic synapse | cellular component | A synapse that uses glutamate as a neurotransmitter. [GOC:dos] |
| cholinergic synapse | cellular component | A synapse that uses acetylcholine as a neurotransmitter. [GOC:dos] |
Active In
This protein is active in 3 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| synapse | cellular component | The junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
Involved In
This protein is involved in 13 target(s):
| Target | Category | Definition |
|---|
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of adenylyl cyclase activity and a subsequent change in the intracellular concentration of cyclic AMP (cAMP). [GOC:mah, GOC:signaling, ISBN:0815316194] |
| phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway | biological process | A phospholipase C-activating G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| G protein-coupled acetylcholine receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a ligand binding to an acetylcholine receptor on the surface of a target cell, and ends with regulation of a downstream cellular process, e.g. transcription. [GOC:mah, ISBN:0815316194] |
| nervous system development | biological process | The process whose specific outcome is the progression of nervous tissue over time, from its formation to its mature state. [GOC:dgh] |
| regulation of heart contraction | biological process | Any process that modulates the frequency, rate or extent of heart contraction. Heart contraction is the process in which the heart decreases in volume in a characteristic way to propel blood through the body. [GOC:dph, GOC:go_curators, GOC:tb] |
| response to virus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a virus. [GOC:hb] |
| G protein-coupled serotonin receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a G protein-coupled serotonin receptor binding to one of its physiological ligands. [GOC:mah] |
| presynaptic modulation of chemical synaptic transmission | biological process | Any process, acting in the presynapse that results in modulation of chemical synaptic transmission. [GOC:dos] |
| regulation of smooth muscle contraction | biological process | Any process that modulates the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway | biological process | An adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway initiated by acetylcholine binding to its receptor, and ending with the regulation of a downstream cellular process. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| chemical synaptic transmission | biological process | The vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435] |