The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
1732545 |
27 |
Phenyl-substituted analogues of oxotremorine as muscarinic antagonists. |
University of Uppsala |
1995893 |
81 |
Muscarinic cholinergic agonists and antagonists of the 3-(3-alkyl-1,2,4-oxadiazol-5-yl)-1,2,5,6-tetrahydropyridine type. Synthesis and structure-activity relationships. |
Ferrosan |
2299626 |
18 |
Beta-lactam analogues of oxotremorine. 3- and 4-methyl-substituted 2-azetidinones. |
University of Uppsala |
2258904 |
21 |
Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. |
Uppsala University |
3346873 |
24 |
Derivatives of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide. |
University of Uppsala |
3336015 |
8 |
Dimethylsulfonium and thiolanium analogues of the muscarinic agent oxotremorine. |
University of California |
3494849 |
3 |
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent. |
TBA |
12113806 |
40 |
Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists. |
Ghent University |
11354386 |
90 |
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands. |
University of Mainz |
27876250 |
60 |
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH |
Jagiellonian University Medical College |
27939174 |
84 |
Challenges in the development of an M |
Vanderbilt University Medical Center |
27839919 |
192 |
Decahydrobenzoquinolin-5-one sigma receptor ligands: Divergent development of both sigma 1 and sigma 2 receptor selective examples. |
University of Kansas |
27185330 |
60 |
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. |
Vanderbilt University Medical Center |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
Jagiellonian University Medical College |
26428869 |
7 |
Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M(1) and M(4) muscarinic acetylcholine receptors agonists. |
Sumitomo Dainippon Pharma |
26471092 |
23 |
Molecular hybridization yields triazole bronchodilators for the treatment of COPD. |
Pfizer |
26299349 |
66 |
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists. |
Eli Lilly |
25893046 |
77 |
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5. |
Bristol-Myers Squibb |
24980056 |
44 |
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites. |
Universit£ |
24856064 |
9 |
Discovery of N-substituted 7-azaindoline derivatives as potent, orally available M1 and M4 muscarinic acetylcholine receptors selective agonists. |
Dainippon Sumitomo Pharma |
25275964 |
171 |
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). |
Universit£ |
25147929 |
105 |
Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). |
Vanderbilt University Medical Center |
24852118 |
7 |
Discovery of N-sulfonyl-7-azaindoline derivatives as potent, orally available and selective M(4) muscarinic acetylcholine receptor agonists. |
Dainippon Sumitomo Pharma |
24805037 |
380 |
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. |
Adamed |
24690494 |
92 |
Antagonists of the kappa opioid receptor. |
The Scripps Research Institute |
18077164 |
40 |
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. |
Universit£ |
24900656 |
9 |
Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists. |
Dainippon Sumitomo Pharma |
23379472 |
187 |
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists. |
University of Arkansas For Medical Sciences |
23200253 |
67 |
Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism. |
Vanderbilt University Medical Center |
23177787 |
59 |
Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
Vanderbilt University Medical Center |
13678406 |
7 |
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. |
The University of Toledo |
22738637 |
19 |
Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor. |
Vanderbilt University Medical Center |
21036043 |
78 |
The discovery of new spirocyclic muscarinic M3 antagonists. |
Astrazeneca |
20709550 |
80 |
The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists. |
Glaxosmithkline |
20483611 |
89 |
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR. |
Glaxosmithkline |
20483599 |
81 |
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling. |
Glaxosmithkline |
19896386 |
85 |
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation. |
Universit£ |
19928767 |
88 |
Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure. |
Universita Di Firenze |
18543900 |
105 |
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists. |
Universit£ |
18595721 |
32 |
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics. |
Alma Mater Studiorum-University of Bologna |
18455407 |
125 |
Muscarinic antagonists with multiple stereocenters: Synthesis, affinity profile and functional activity of isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine sulfoxide derivatives. |
Universit£ |
| 20 |
Design, synthesis and biological activity of some 4-DAMP- related compounds |
TBA |
23084435 |
17 |
Synthesis of N-phenyl-N-(3-(piperidin-1-yl)propyl)benzofuran-2-carboxamides as new selective ligands for sigma receptors. |
Savannah State University |
22959245 |
175 |
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs). |
The University of Sydney |
23062550 |
59 |
Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists. |
Vanderbilt University Medical Center |
22335555 |
43 |
1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate. |
Neuraxon |
24900202 |
38 |
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists. |
TBA |
22677319 |
64 |
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential. |
H. Lundbeck |
22749871 |
92 |
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012. |
Vanderbilt University Medical Center |
22243489 |
75 |
1,4-dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists. |
Universit£ |
22607684 |
50 |
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands. |
The University of Sydney |
22313227 |
78 |
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype. |
National Institute of Mental Health |
22507963 |
73 |
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. |
Vanderbilt University Medical Center |
22148921 |
48 |
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c |
Cephalon |
21207959 |
69 |
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging. |
National Institute of Mental Health |
20684563 |
176 |
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. |
H. Lundbeck |
19963380 |
38 |
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. |
Hunter College and The Graduate Center of The City University of New York |
18468904 |
48 |
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand. |
Purdue University |
18395442 |
5 |
Diphenidol-related diamines as novel muscarinic M4 receptor antagonists. |
University of Bologna |
18042383 |
20 |
Design and synthesis of a fluorescent muscarinic antagonist. |
Pfizer |
17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
17889543 |
90 |
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes. |
Universit£ |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
14998318 |
112 |
Selective optimization of side activities: another way for drug discovery. |
Prestwick Chemical |
11831911 |
15 |
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes. |
Banyu Tsukuba Research Institute |
9986705 |
290 |
Identification and characterization of m1 selective muscarinic receptor antagonists1. |
Warner-Lambert |
9622546 |
109 |
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. |
National Institute of Diabetes and Digestive and Kidney Diseases |
1956033 |
121 |
Synthesis, molecular modeling studies, and muscarinic receptor activity of azaprophen analogues. |
Research Triangle Institute |
2153827 |
12 |
Functionalized congener approach for the design of novel muscarinic agents. Synthesis and pharmacological evaluation of N-methyl-N-[4-(1-pyrrolidinyl)-2-butynyl] amides. |
Niddk |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
9873472 |
102 |
Identification and characterization of m4 selective muscarinic antagonists. |
Parke-Davis Pharmaceutical Research |
| 24 |
1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonists |
TBA |
22226656 |
75 |
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test. |
Cephalon |
22197142 |
42 |
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012. |
Vanderbilt University Medical Center |
22030026 |
13 |
Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator. |
Vanderbilt University Medical Center |
21930376 |
92 |
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. |
Vanderbilt University Medical Center |
21870878 |
61 |
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. |
Pfizer |
21788137 |
33 |
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands. |
The University of Sydney |
21865048 |
29 |
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A. |
Dainippon Sumitomo Pharma |
21194936 |
39 |
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. |
Vanderbilt Institute of Chemical Biology/Chemical Synthesis Core |
21195614 |
56 |
Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. |
Pfizer |
21146989 |
46 |
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands. |
The University of Sydney |
20812727 |
157 |
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography. |
National Institute of Mental Health |
20801651 |
25 |
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. |
Vanderbilt University Medical Center |
20202841 |
47 |
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists. |
Vanderbilt University Medical Center |
20043678 |
92 |
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models. |
Pfizer |
19646882 |
72 |
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. |
University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School and The Informatics Institute of Umdnj |
19616432 |
176 |
Design, synthesis and evaluation of N-[(3S)-pyrrolidin-3-yl]benzamides as selective noradrenaline reuptake inhibitors: CNS penetration in a more polar template. |
Pfizer |
7673927 |
6 |
Isolation and Structure of Two Novel Muscarinic Receptor Antagonists |
TBA |
| 32 |
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053) |
TBA |
| 44 |
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists |
TBA |
| 37 |
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists. |
TBA |
| 31 |
3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonists |
TBA |
| 74 |
New indole derivatives as potent and selective serotonin uptake inhibitors |
TBA |
19208472 |
52 |
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists. |
Novartis Institutes For Biomedical Research |
18829311 |
74 |
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. |
Vanderbilt University Medical Center |
18805692 |
99 |
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. |
Vanderbilt University Medical Center |
18701276 |
97 |
Highly functionalized 7-azaindoles as selective PPAR gamma modulators. |
Merck Research Laboratories |
16038549 |
20 |
Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674. |
Mitsubishi Pharma |
15844951 |
5 |
Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata. |
Mitsubishi Pharma |
17571866 |
49 |
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography. |
National Institute of Mental Health |
17317171 |
91 |
M4 agonists/5HT7 antagonists with potential as antischizophrenic drugs: serominic compounds. |
University of Strathclyde |
16970392 |
91 |
Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity. |
Tsukuba Research Institute |
16722655 |
28 |
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. |
Pfizer |
16722631 |
87 |
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
Predix Pharmaceuticals |
16458504 |
37 |
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand. |
Columbia University College of Physicians and Surgeons |
16392798 |
46 |
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. |
Columbia University College of Physicians and Surgeons |
16143528 |
213 |
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. |
Columbia University College of Physicians and Surgeons |
14643338 |
124 |
Binding of beta-carbolines at 5-HT(2) serotonin receptors. |
Virginia Commonwealth University |
12747793 |
32 |
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. |
University of North Carolina At Chapel Hill |
12361399 |
17 |
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding. |
Universita Di Camerino |
11741475 |
56 |
Design, synthesis, and biological characterization of bivalent 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as selective muscarinic agonists. |
The University of Toledo |
11708906 |
15 |
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators. |
University of Bologna |
11378358 |
254 |
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. |
Columbia University College of Physicians and Surgeons |
32374602 |
190 |
Novel Potent Muscarinic Receptor Antagonists: Investigation on the Nature of Lipophilic Substituents in the 5- and/or 6-Positions of the 1,4-Dioxane Nucleus. |
Universit£ |
32227883 |
40 |
Isolation and Synthesis of Veranamine, an Antidepressant Lead from the Marine Sponge |
University of Mississippi |
31787491 |
54 |
Discovery of structurally distinct tricyclic M |
Vanderbilt University |
31784320 |
31 |
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M |
Vanderbilt University |
32233403 |
135 |
Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M |
University of Regensburg |
11012031 |
57 |
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency. |
Schering-Plough Research Institute |
27476142 |
104 |
Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition. |
Vanderbilt University School of Medicine |
27503678 |
32 |
Ligand-based virtual screen for the discovery of novel M5 inhibitor chemotypes. |
Vanderbilt University |
10891110 |
87 |
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors. |
National Institute of Diabetes and Digestive and Kidney Diseases |
32342685 |
325 |
Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D |
National Institute of Neurological Disorders and Stroke |
10498210 |
27 |
A new class of selective and potent inhibitors of neuronal nitric oxide synthase. |
Pfizer |
31074983 |
202 |
Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M |
University of Regensburg |
31021617 |
136 |
Leveraging a Low-Affinity Diazaspiro Orthosteric Fragment to Reduce Dopamine D |
University of Pennsylvania |
31248774 |
45 |
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M |
Vanderbilt University |
30580918 |
36 |
Novel M |
Vanderbilt University |
30554957 |
105 |
Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M |
University of Kentucky |
31913038 |
13 |
Preventing Morphine-Seeking Behavior through the Re-Engineering of Vincamine's Biological Activity. |
University of Florida |
9651157 |
52 |
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. |
Warner-Lambert |
9438027 |
30 |
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. |
Novo Nordisk |
9435896 |
36 |
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. |
Smithkline Beecham Pharmaceuticals |
30106578 |
10 |
Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts. |
TBA |
31620230 |
283 |
3-Amino-chromanes and Tetrahydroquinolines as Selective 5-HT |
University of Minnesota Twin Cities |
31223452 |
49 |
Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres. |
Pfizer |
24074052 |
24 |
Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor. |
Monash University |
23523385 |
73 |
Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods. |
Walter Reed Army Institute of Research |
7783150 |
33 |
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. |
Royal Danish School of Pharmacy |
21075638 |
105 |
Synthesis and pharmacological properties of novel hydrophilic 5-HT4 receptor antagonists. |
Drug Discovery Laboratory |
32353859 |
59 |
A SARS-CoV-2 protein interaction map reveals targets for drug repurposing. |
Qbi Covid-19 Research Group (Qcrg) |
17880057 |
131 |
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs. |
Solvay Pharma |
17084634 |
24 |
Dioxane and oxathiane nuclei: suitable substructures for muscarinic agonists. |
Universit£ |
16539379 |
95 |
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. |
Universit£ |
16153841 |
24 |
Activity and QSAR study of baogongteng A and its derivatives as muscarinic agonists. |
Shanghai Second Medical University |
12593665 |
188 |
Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists. |
Johannes Gutenberg-University of Mainz |
12086495 |
130 |
Synthesis and pharmacology of benzoxazines as highly selective antagonists at M(4) muscarinic receptors. |
Pfizer |
9371246 |
159 |
Antimuscarinic 3-(2-furanyl)quinuclidin-2-ene derivatives: synthesis and structure-activity relationships. |
Uppsala University |
8765510 |
100 |
3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists. |
Uppsala University |
3712371 |
49 |
A novel class of conformationally restricted heterocyclic muscarinic agonists. |
TBA |
30258541 |
94 |
VU6007477, a Novel M |
Vanderbilt Univercity |
30128067 |
12 |
Allosteric Modulators of the M4 Muscarinic Acetylcholine Receptor. |
Usona Institute |
29089231 |
49 |
Challenges in the development of an M |
Vanderbilt University School of Medicine |
30052039 |
172 |
Design, Synthesis, and Pharmacological Evaluation of Second-Generation Tetrahydroisoquinoline-Based CXCR4 Antagonists with Favorable ADME Properties. |
Emory University |
29656199 |
148 |
Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties. |
University of Texas At Austin |
29795757 |
100 |
Discovery of |
Emory University |
29348805 |
56 |
Synthesis and SAR of 1,2,3,4-Tetrahydroisoquinoline-Based CXCR4 Antagonists. |
Emory University |
28609709 |
75 |
Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments. |
Universit£ |
28633897 |
73 |
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. |
Vanderbilt University School of Medicine |
28388054 |
72 |
Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M |
University of Regensburg |
29589445 |
154 |
1-[3-(4-Butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1) as a Model for the Rational Design of a Novel Class of Brain Penetrant Ligands with High Affinity and Selectivity for Dopamine D |
Universit£ |
28866269 |
61 |
Discovery of a novel, CNS penetrant M |
Vanderbilt University |
1674541 |
24 |
Conformational properties of semirigid antipsychotic drugs: the pharmacophore for dopamine D-2 antagonist activity. |
Harvard Medical School |
28522253 |
83 |
Challenges in the development of an M |
Vanderbilt University School of Medicine |
1560441 |
35 |
Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues). |
Institute of Research |
28442253 |
68 |
Optimization of M |
Vanderbilt University Medical Center |
28598634 |
26 |
Design and Synthesis of?- and?-Lactam M |
Pfizer |
28427812 |
74 |
Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype. |
Vanderbilt University School of Medicine |
26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
23548908 |
1 |
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis. |
University of Washington |
26077890 |
33 |
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids. |
Tehran University of Medical Sciences |
26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
26174207 |
21 |
Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase. |
The Johns Hopkins University School of Medicine |
16480269 |
9 |
Application of Fragment Screening and Fragment Linking to the Discovery of Novel Thrombin Inhibitors. |
Astex |