The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 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£ |
| 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 |
| 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 |
| | 44 |
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists |
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 |
| 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 |
| 11012031 |
57 |
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency. |
Schering-Plough Research Institute |
| 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 |
| 10498210 |
27 |
A new class of selective and potent inhibitors of neuronal nitric oxide synthase. |
Pfizer |
| 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 |
| 7783150 |
33 |
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. |
Royal Danish School Of Pharmacy |
| 1560441 |
35 |
Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues). |
Institute Of Research |
| 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 |
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