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1. Full Text Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists
by Cheng, Jianjun and McCorvy, John D and Giguere, Patrick M and Zhu, Hu and Kenakin, Terry and Roth, Bryan L and Kozikowski, Alan P
Journal of Medicinal Chemistry, ISSN 0022-2623, 11/2016, Volume 59, Issue 21, pp. 9866 - 9880
On the basis of the structural similarity of our previous 5-HT2C agonists with the melatonin receptor agonist tasimelteon and the putative biological... 
DRUG | POTENT | CHEMISTRY, MEDICINAL | LIGANDS | MODELS | DISEASE | TRANSDUCTION | AGENTS | IDENTIFICATION | Dose-Response Relationship, Drug | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Molecular Structure | Structure-Activity Relationship | Drug Discovery | Serotonin 5-HT2 Receptor Agonists - chemistry
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2. Full Text Discovery of N‑Substituted (2-Phenylcyclopropyl)methylamines as Functionally Selective Serotonin 2C Receptor Agonists for Potential Use as Antipsychotic Medications
by Zhang, Guiping and Cheng, Jianjun and McCorvy, John D and Lorello, Paul J and Caldarone, Barbara J and Roth, Bryan L and Kozikowski, Alan P
Journal of Medicinal Chemistry, ISSN 0022-2623, 07/2017, Volume 60, Issue 14, pp. 6273 - 6288
A series of N-substituted (2-phenylcyclopropyl)­methylamines were designed and synthesized, with the aim of finding serotonin 2C (5-HT2C)-selective agonists... 
DRUG | PHENCYCLIDINE | DESIGN | CHEMISTRY, MEDICINAL | METABOLISM | EFFICACY | MODELS | BETA-ARRESTINS | OPTIMIZATION | IDENTIFICATION | 5-HT2B RECEPTORS | Benzylamines - chemical synthesis | Receptor, Serotonin, 5-HT2B - metabolism | Stereoisomerism | Humans | Receptor, Serotonin, 5-HT2C - metabolism | beta-Arrestins - metabolism | Male | Methylamines - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Antipsychotic Agents - chemical synthesis | Hyperkinesis - drug therapy | Cyclopropanes - chemistry | Cyclopropanes - chemical synthesis | HEK293 Cells | Hyperkinesis - chemically induced | Methylamines - chemistry | Methylamines - pharmacology | Cyclopropanes - pharmacology | Mice, Inbred C57BL | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - chemistry | Benzylamines - chemistry | Animals | Antipsychotic Agents - chemistry | Antipsychotic Agents - pharmacology | Benzylamines - pharmacology
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3. Full Text Synthesis and biological evaluation of new naphtho- and quinolinocyclopentane derivatives as potent melatoninergic (MT1/MT2) and serotoninergic (5-HT2C) dual ligands
by Duroux, Romain and Rami, Marouan and Landagaray, Elodie and Ettaoussi, Mohamed and Caignard, Daniel-Henri and Delagrange, Philippe and Melnyk, Patricia and Yous, Saïd
European Journal of Medicinal Chemistry, ISSN 0223-5234, 12/2017, Volume 141, pp. 552 - 566
We recently reported a series of naphthofuranic compounds as constrained agomelatine analogues. Herein, in order to explore alternative ethyl amide side chain... 
Levogyre | Dextrogyre | Melatonin | Agomelatine | Serotonin | DESIGN | CHEMISTRY, MEDICINAL | SERIES | RECEPTOR AGONISTS | PLASMODIUM-FALCIPARUM | RAMELTEON | MALARIA | SECRETION | INHIBITOR | PHARMACOLOGICAL EVALUATION | Receptor, Melatonin, MT2 - agonists | Cell Line | Cricetinae | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Cyclopentanes - chemistry | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Cyclopentanes - pharmacology | Serotonin 5-HT2 Receptor Agonists - chemistry | Dose-Response Relationship, Drug | Receptor, Melatonin, MT1 - agonists | Animals | Ligands | Molecular Structure | Cyclopentanes - chemical synthesis | Medicinal Chemistry | Chemical Sciences
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4. Full Text Optimization of 2‑Phenylcyclopropylmethylamines as Selective Serotonin 2C Receptor Agonists and Their Evaluation as Potential Antipsychotic Agents
by Cheng, Jianjun and Giguère, Patrick M and Onajole, Oluseye K and Lv, Wei and Gaisin, Arsen and Gunosewoyo, Hendra and Schmerberg, Claire M and Pogorelov, Vladimir M and Rodriguiz, Ramona M and Vistoli, Giulio and Wetsel, William C and Roth, Bryan L and Kozikowski, Alan P
Journal of Medicinal Chemistry, ISSN 0022-2623, 02/2015, Volume 58, Issue 4, pp. 1992 - 2002
The discovery of a new series of compounds that are potent, selective 5-HT2C receptor agonists is described herein as we continue our efforts to optimize the... 
LORCASERIN | OBESITY | CHEMISTRY, MEDICINAL | LIGANDS | IN-VIVO | RATIONAL DRUG DESIGN | IDENTIFICATION | BINDING | 5-HT2C AGONIST | Humans | Microsomes, Liver - metabolism | Receptor, Serotonin, 5-HT2C - metabolism | Allyl Compounds - chemistry | Cytochrome P-450 Enzyme System - metabolism | Male | Methylamines - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Antipsychotic Agents - chemical synthesis | Dose-Response Relationship, Drug | Microsomes, Liver - drug effects | Microsomes, Liver - enzymology | Molecular Structure | Methylamines - chemistry | Methylamines - pharmacology | Locomotion - drug effects | Allyl Compounds - chemical synthesis | Caco-2 Cells | Mice, Inbred C57BL | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Models, Molecular | Allyl Compounds - pharmacology | Serotonin 5-HT2 Receptor Agonists - chemistry | Amphetamine | Animals | Antipsychotic Agents - chemistry | Mice | Antipsychotic Agents - pharmacology
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5. Full Text Multiparameter Optimization in CNS Drug Discovery: Design of Pyrimido[4,5‑d]azepines as Potent 5‑Hydroxytryptamine 2C (5-HT2C) Receptor Agonists with Exquisite Functional Selectivity over 5‑HT2A and 5‑HT2B Receptors
by Storer, R. Ian and Brennan, Paul E and Brown, Alan D and Bungay, Peter J and Conlon, Kelly M and Corbett, Matthew S and DePianta, Robert P and Fish, Paul V and Heifetz, Alexander and Ho, Danny K. H and Jessiman, Alan S and McMurray, Gordon and de Oliveira, Cesar Augusto F and Roberts, Lee R and Root, James A and Shanmugasundaram, Veerabahu and Shapiro, Michael J and Skerten, Melanie and Westbrook, Dominique and Wheeler, Simon and Whitlock, Gavin A and Wright, John
Journal of Medicinal Chemistry, ISSN 0022-2623, 06/2014, Volume 57, Issue 12, pp. 5258 - 5269
A series of 4-substituted pyrimido[4,5-d]azepines that are potent, selective 5-HT2C receptor partial agonists is described. A rational medicinal chemistry... 
IN-VITRO | OBESITY | CHEMISTRY, MEDICINAL | PROTEIN-COUPLED RECEPTOR | ANTIOBESITY AGENTS | CENTRAL-NERVOUS-SYSTEM | IDENTIFICATION | BLOOD-BRAIN-BARRIER | BINDING | P-GLYCOPROTEIN | URINARY-INCONTINENCE | Cricetulus | Pyrimidines - chemical synthesis | Receptor, Serotonin, 5-HT2B - metabolism | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Pyrimidines - chemistry | Azepines - chemistry | Drug Design | Madin Darby Canine Kidney Cells | CHO Cells | Central Nervous System Agents - chemistry | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Azepines - chemical synthesis | Permeability | Pyrimidines - pharmacology | Serotonin 5-HT2 Receptor Agonists - chemistry | Blood-Brain Barrier - metabolism | Azepines - pharmacology | Animals | Central Nervous System Agents - pharmacology | Dogs | Central Nervous System Agents - chemical synthesis | Receptor, Serotonin, 5-HT2A - metabolism | Urinary Incontinence, Stress - drug therapy
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6. Full Text Synthesis and in vitro evaluation of [18F]FECIMBI-36: A potential agonist PET ligand for 5-HT2A/2C receptors
by Prabhakaran, Jaya and Underwood, Mark D and Kumar, J.S. Dileep and Simpson, Norman R and Kassir, Suham A and Bakalian, Mihran J and Mann, J. John and Arango, Victoria
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 09/2015, Volume 25, Issue 18, pp. 3933 - 3936
Radiosynthesis and in vitro evaluation of [ F]-2-(4-bromo-2,5-dimethoxyphenyl)- -(2-(2-fluoroethoxy)benzyl)ethanamine, ([ F]FECIMBI-36) or ([ F] ), a potential... 
Agonist | 5-HT | 5HT2A/2CR | Radiotracer | PET | CHEMISTRY, MEDICINAL | HUMAN BRAIN | RADIOLIGAND | 5HT(2A/2C)R | SEROTONIN RECEPTORS | CHEMISTRY, ORGANIC | RADIOTRACERS | H-3 KETANSERIN | BINDING | Ethylamines - pharmacology | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Ethylamines - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Positron-Emission Tomography | Structure-Activity Relationship | Serotonin 5-HT2 Receptor Agonists - chemistry | Dose-Response Relationship, Drug | Ligands | Molecular Structure | Ethylamines - chemistry | Fluorine Radioisotopes - chemistry | Receptor, Serotonin, 5-HT2A - metabolism | Serotonin 5-HT2 Receptor Agonists - metabolism | Fluorine Radioisotopes - pharmacology | 2CR | 5HT2A
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7. Full Text Synthesis and Structure–Activity Relationships of N‑Benzyl Phenethylamines as 5‑HT2A/2C Agonists
by Hansen, Martin and Phonekeo, Karina and Paine, James S and Leth-Petersen, Sebastian and Begtrup, Mikael and Bräuner-Osborne, Hans and Kristensen, Jesper L
ACS Chemical Neuroscience, ISSN 1948-7193, 01/2014, Volume 5, Issue 3, pp. 243 - 249
N-Benzyl substitution of 5-HT2A receptor agonists of the phenethylamine structural class of psychedelics (such as 4-bromo-2,5-dimethoxyphenethylamine, often... 
selectivity | Serotonin | N -benzyl phenethylamines | ACID DIETHYLAMIDE | CHEMISTRY, MEDICINAL | SAFETY | BIOCHEMISTRY & MOLECULAR BIOLOGY | MODEL | N-benzyl phenethylamines | NEUROSCIENCES | S-HT2A receptor agonist | PSILOCYBIN | BIOLOGY | CLUSTER HEADACHE | RECEPTORS | BINDING | DERIVATIVES | MYSTICAL-TYPE EXPERIENCES | Binding, Competitive | Serotonin 5-HT2 Receptor Agonists - pharmacokinetics | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Dose-Response Relationship, Drug | Phenethylamines - pharmacokinetics | Phenethylamines - chemical synthesis | HEK293 Cells | Molecular Structure | Radioligand Assay | Inositol Phosphates - metabolism | Receptor, Serotonin, 5-HT2A - metabolism
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8. Full Text Preclinical Safety Assessment of the 5-HT2A Receptor Agonist PET Radioligand [11C]Cimbi-36
by Ettrup, Anders and Holm, Søren and Hansen, Martin and Wasim, Muhammad and Santini, Martin Andreas and Palner, Mikael and Madsen, Jacob and Svarer, Claus and Kristensen, Jesper Langgaard and Knudsen, Gitte Moos
Molecular Imaging and Biology, ISSN 1536-1632, 8/2013, Volume 15, Issue 4, pp. 376 - 383
[11C]Cimbi-36 was recently developed as an agonist radioligand for brain imaging of serotonin 2A receptors (5-HT2A) with positron emission tomography (PET).... 
Porcine | Medicine & Public Health | Serotonin receptors | Radiation dosimetry | Imaging / Radiology | PET | Head-twitch response | Hallucinogenic | POSITRON-EMISSION-TOMOGRAPHY | IN-VIVO | SEROTONIN | RELEASE | BINDING | RADIOLOGY, NUCLEAR MEDICINE & MEDICAL IMAGING | Serotonin 5-HT2 Receptor Agonists - pharmacokinetics | Tissue Distribution - drug effects | Benzylamines - adverse effects | Benzylamines - chemical synthesis | Humans | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - adverse effects | Phenethylamines - chemistry | Rats | Positron-Emission Tomography | Serotonin 5-HT2 Receptor Agonists - chemistry | Benzylamines - chemistry | Animals | Phenethylamines - pharmacokinetics | Phenethylamines - adverse effects | Phenethylamines - chemical synthesis | Ligands | Radiometry | Whole Body Imaging | Mice | Benzylamines - pharmacokinetics | Receptor, Serotonin, 5-HT2A - metabolism | Dose-Response Relationship, Radiation | Sus scrofa
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9. Full Text Synthesis and pharmacological evaluation of piperidine (piperazine)-substituted benzoxazole derivatives as multi-target antipsychotics
by Huang, Ling and Zhang, Xiaohua and Zhang, Wenjun and Yin, Lei and Chen, Bangyin and Song, Jinchun
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 11/2015, Volume 25, Issue 22, pp. 5299 - 5305
The present study describes the optimization of a series of novel benzoxazole–piperidine (piperazine) derivatives combining high dopamine D and serotonin 5-HT... 
Antipsychotic | Piperidine | Piperazine | Benzoxazole | DRUG | CHEMISTRY, MEDICINAL | HALOPERIDOL | CHEMISTRY, ORGANIC | SCHIZOPHRENIA | RECEPTOR | DISCOVERY | POTENT | DOPAMINE D-3 | LIGANDS | INDUCED WEIGHT-GAIN | BLOCKADE | Antipsychotic Agents - toxicity | Humans | Serotonin 5-HT1 Receptor Agonists - pharmacology | Piperazines - toxicity | Serotonin 5-HT1 Receptor Agonists - toxicity | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Antipsychotic Agents - chemical synthesis | Piperidines - pharmacology | Swine | Serotonin 5-HT2 Receptor Agonists - toxicity | Potassium Channel Blockers - toxicity | Potassium Channel Blockers - pharmacology | Piperidines - toxicity | Receptors, Dopamine D2 - agonists | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Rats | Serotonin 5-HT1 Receptor Agonists - chemical synthesis | Piperidines - chemical synthesis | Potassium Channel Blockers - chemical synthesis | Piperazines - pharmacology | Ether-A-Go-Go Potassium Channels - antagonists & inhibitors | Oxazoles - chemical synthesis | Patch-Clamp Techniques | Animals | Oxazoles - toxicity | Piperazines - chemical synthesis | Mice | Oxazoles - pharmacology | Antipsychotic Agents - pharmacology | Schizophrenia - drug therapy | Analysis | Antipsychotic drugs
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10. Full Text Selective 5-HT2C receptor agonists: Design and synthesis of pyridazine-fused azepines
by Green, Martin P and McMurray, Gordon and Storer, R. Ian
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 08/2016, Volume 26, Issue 16, pp. 4117 - 4121
Heterocycle-fused azepines are discussed as potent 5-HT receptor agonists with excellent selectivity over 5-HT agonism. Synthesis and structure activity... 
Urinary incontinence | Obesity | 5-HT2C receptor agonists | Pyridazino[3,4-d]azepines | CNS penetration | CHEMISTRY, MEDICINAL | PERMEABILITY | CHEMISTRY, ORGANIC | BLOOD-BRAIN-BARRIER | DISCOVERY | P-GLYCOPROTEIN | IN-VITRO | LORCASERIN | POTENT | DRUGS | CENTRAL-NERVOUS-SYSTEM | Receptor, Serotonin, 5-HT2B - metabolism | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism | Azepines - chemical synthesis | Structure-Activity Relationship | Serotonin 5-HT2 Receptor Agonists - chemistry | Pyridazines - chemistry | Receptor, Serotonin, 5-HT2B - chemistry | Animals | Azepines - chemistry | ATP-Binding Cassette, Sub-Family B, Member 1 - genetics | Receptor, Serotonin, 5-HT2C - chemistry | Azepines - metabolism | Dogs | Drug Design | Madin Darby Canine Kidney Cells | Protein Binding | Serotonin 5-HT2 Receptor Agonists - metabolism
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11. Full Text Synthesis and pharmacological evaluation of N-benzyl substituted 4-bromo-2,5-dimethoxyphenethylamines as 5-HT2A/2C partial agonists
by Hansen, Martin and Jacobsen, Stine Engesgaard and Plunkett, Shane and Liebscher, Gudrun Eckhard and McCorvy, John D and Bräuner-Osborne, Hans and Kristensen, Jesper Langgaard
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 07/2015, Volume 23, Issue 14, pp. 3933 - 3937
-Benzyl substitution of phenethylamine 5-HT receptor agonists has dramatic effects on binding affinity, receptor selectivity and agonist activity. In this... 
5-HT2A agonists | Selectivity | Structure activity relations | Serotonin | N-Benzyl phenethylamines | DESIGN | CHEMISTRY, MEDICINAL | SERIES | ANALOGS | RECEPTOR AGONISTS | BIOCHEMISTRY & MOLECULAR BIOLOGY | CHEMISTRY, ORGANIC | PET RADIOLIGAND | Dimethoxyphenylethylamine - analogs & derivatives | Drug Evaluation, Preclinical - methods | Chemistry Techniques, Synthetic | Receptor, Serotonin, 5-HT2B - metabolism | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | HEK293 Cells - drug effects | Serotonin 5-HT2 Receptor Agonists - chemistry | Fluorescence Resonance Energy Transfer | Dimethoxyphenylethylamine - chemistry
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12. Full Text Convergent 18 F-labeling and evaluation of N-benzyl-phenethylamines as 5-HT 2A receptor PET ligands
by Petersen, Ida Nymann and Villadsen, Jonas and Hansen, Hanne Demant and Jensen, Anders A and Lehel, Szabolcs and Gillings, Nic and Herth, Matthias M and Knudsen, Gitte M and Kristensen, Jesper L
Bioorganic & medicinal chemistry, ISSN 0968-0896, 11/2016, Volume 24, Issue 21, pp. 5353 - 5356
Positron emission tomography (PET) investigations of the 5-HT receptor (5-HT R) system can be used as a research tool in diseases such as depression,... 
Radiopharmaceuticals - chemistry | Ethylamines - pharmacology | Humans | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Ethylamines - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Positron-Emission Tomography | Structure-Activity Relationship | Radiopharmaceuticals - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - chemistry | Benzyl Compounds - chemistry | Dose-Response Relationship, Drug | Benzyl Compounds - pharmacology | Ligands | Molecular Structure | Benzyl Compounds - chemical synthesis | Ethylamines - chemistry | Fluorine Radioisotopes | Receptor, Serotonin, 5-HT2A - metabolism | Radiopharmaceuticals - pharmacology
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13. Full Text In vivo evaluation of [ 18 F]FECIMBI-36, an agonist 5-HT 2A/2C receptor PET radioligand in nonhuman primate
by Prabhakaran, Jaya and Solingapuram Sai, Kiran Kumar and Zanderigo, Francesca and Rubin-Falcone, Harry and Jorgensen, Matthew J and Kaplan, Jay R and Tooke, Katharine I and Mintz, Akiva and Mann, J John and Kumar, J S Dileep
Bioorganic & medicinal chemistry letters, ISSN 0960-894X, 01/2017, Volume 27, Issue 1, pp. 21 - 23
We recently reported the radiosynthesis and in vitro evaluation of [ F]-2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-(2-fluoroethoxy)benzyl)ethanamine, ([... 
Ethylamines - pharmacology | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Cercopithecus aethiops | Ethylamines - chemical synthesis | Male | Serotonin 5-HT2 Receptor Agonists - pharmacology | Positron-Emission Tomography | Structure-Activity Relationship | Serotonin 5-HT2 Receptor Agonists - chemistry | Dose-Response Relationship, Drug | Magnetic Resonance Imaging | Animals | Ligands | Molecular Structure | Ethylamines - chemistry | Fluorine Radioisotopes - chemistry | Receptor, Serotonin, 5-HT2A - metabolism | Fluorine Radioisotopes - pharmacology
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14. Full Text Identification of optically active pyrimidine derivatives as selective 5-HT 2C modulators
by Kim, Juhyeon and Jo, Hanbyeol and Lee, Hyunseung and Choo, Hyunah and Kim, Hak Joong and Pae, Ae Nim and Cho, Yong Seo and Min, Sun-Joon
Molecules, 09/2017, Volume 22, Issue 9
A series of pyrimidine derivatives - were synthesized and evaluated for their binding affinities towards 5-HT receptors. With regard to designed molecules - ,... 
Optically active | 5-HT2C receptor | Selectivity | Binding affinity | Enzymatic kinetic resolution | Pyrimidine | Cricetulus | Pyrimidines - chemical synthesis | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Models, Molecular | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Pyrimidines - pharmacology | Pyrimidines - chemistry | Serotonin 5-HT2 Receptor Agonists - chemistry | Animals | Molecular Structure | CHO Cells
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15. Full Text Alpha-ethyltryptamines as dual dopamine–serotonin releasers
by Blough, Bruce E and Landavazo, Antonio and Partilla, John S and Decker, Ann M and Page, Kevin M and Baumann, Michael H and Rothman, Richard B
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 10/2014, Volume 24, Issue 19, pp. 4754 - 4758
The dopamine (DA), serotonin (5-HT), and norepinephrine (NE) transporter releasing activity and serotonin-2A (5-HT ) receptor agonist activity of a series of... 
DA releasers | Tryptamines | 5-HT 2A receptor | 5-HT releasers | BIOGENIC-AMINE TRANSPORTERS | CHEMISTRY, MEDICINAL | COCAINE ADDICTION | RHESUS-MONKEYS | MEDICATION DEVELOPMENT | CHEMISTRY, ORGANIC | MONOAMINE RELEASERS | PHENTERMINE | DEPENDENCE | DISCRIMINATIVE STIMULUS | FOOD | Tryptamines - chemistry | Tryptamines - chemical synthesis | Humans | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Serotonin 5-HT2 Receptor Agonists - chemistry | Dose-Response Relationship, Drug | Norepinephrine - metabolism | Tryptamines - pharmacology | Serotonin - metabolism | Molecular Structure | Receptor, Serotonin, 5-HT2A - metabolism | Dopamine - metabolism | Serotonin | tryptamines
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16. Full Text Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models
by Cheng, Jianjun and Giguere, Patrick M and Schmerberg, Claire M and Pogorelov, Vladimir M and Rodriguiz, Ramona M and Huang, Xi-Ping and Zhu, Hu and McCorvy, John D and Wetsel, William C and Roth, Bryan L and Kozikowski, Alan P
Journal of Medicinal Chemistry, ISSN 0022-2623, 01/2016, Volume 59, Issue 2, pp. 578 - 591
A series of novel compounds with two halogen substituents have been designed and synthesized to further optimize the 2-phenylcyclopropylmethylamine scaffold in... 
ATYPICAL ANTIPSYCHOTIC-DRUGS | MEDICINAL CHEMISTRY | DESIGN | POTENT | CHEMISTRY, MEDICINAL | MEDICATIONS | LIGANDS | RECEPTOR AGONISTS | SCHIZOPHRENIA | WEIGHT-GAIN | IDENTIFICATION | Central Nervous System Stimulants | Humans | Microsomes, Liver - metabolism | Substrate Specificity | Male | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Schizophrenic Psychology | Hyperkinesis - drug therapy | Brain - metabolism | Drug Design | Catalepsy - chemically induced | Female | Hyperkinesis - chemically induced | Drug Evaluation, Preclinical | Receptor, Serotonin, 5-HT2C - drug effects | Mice, Inbred C57BL | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Dextroamphetamine | Cognition - drug effects | Ether-A-Go-Go Potassium Channels - antagonists & inhibitors | Animals | Recognition (Psychology) - drug effects | Hyperkinesis - psychology | Prepulse Inhibition - drug effects | Mice | Schizophrenia - drug therapy
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17. Full Text Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists
by Fevig, John M and Feng, Jianxin and Rossi, Karen A and Miller, Keith J and Wu, Ginger and Hung, Chen-Pin and Ung, Thao and Malmstrom, Sarah E and Zhang, Ge and Keim, William J and Cullen, Mary Jane and Rohrbach, Kenneth W and Qu, Qinling and Gan, Jinping and Pelleymounter, Mary Ann and Robl, Jeffrey A
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 01/2013, Volume 23, Issue 1, pp. 330 - 335
A series of 2,3,3a,4-tetrahydro-1 -pyrrolo[3,4- ]isoquinolin-5(9b )-ones is described, several examples of which exhibit potent 5-HT agonism with excellent... 
Serotonin | Obesity | 5-HT2c receptor agonist | 5-HT | receptor agonist | LORCASERIN | CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | MICE | FENFLURAMINE | DISCOVERY | Serotonin 5-HT2 Receptor Agonists - pharmacokinetics | Pyrroles - pharmacokinetics | Isoquinolines - pharmacokinetics | Receptor, Serotonin, 5-HT2B - metabolism | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Half-Life | Male | Structure-Activity Relationship | Heterocyclic Compounds, 3-Ring - chemical synthesis | Receptor, Serotonin, 5-HT2A - chemistry | Isoquinolines - chemistry | Heterocyclic Compounds, 3-Ring - pharmacokinetics | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Rats | Rats, Sprague-Dawley | Serotonin 5-HT2 Receptor Agonists - chemistry | Receptor, Serotonin, 5-HT2B - chemistry | Animals | Pyrroles - chemical synthesis | Heterocyclic Compounds, 3-Ring - chemistry | Isoquinolines - chemical synthesis | Receptor, Serotonin, 5-HT2C - chemistry | Pyrroles - chemistry | Receptor, Serotonin, 5-HT2A - metabolism
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18. Full Text 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
by Andrews, Mark D and Fish, Paul V and Blagg, Julian and Brabham, Tiffini K and Brennan, Paul E and Bridgeland, Alison and Brown, Alan D and Bungay, Peter J and Conlon, Kelly M and Edmunds, Nicholas J and Af Forselles, Kerry and Gibbons, Colleen P and Green, Martin P and Hanton, Giles and Holbrook, Mark and Jessiman, Alan S and McIntosh, Karin and McMurray, Gordon and Nichols, Carly L and Root, James A and Storer, R. Ian and Sutton, Michael R and Ward, Robin V and Westbrook, Dominique and Whitlock, Gavin A
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 05/2011, Volume 21, Issue 9, pp. 2715 - 2720
New pyrimido[4,5-d]azepines 7 are disclosed as potent 5-HT receptor agonists. A preferred example, 7b had minimal activation at either the 5-HT or 5-HT... 
Urinary incontinence | Pyrimido[4,5-d]azepines | PF-3246799 | receptor agonists | 5-HT | LORCASERIN | CHEMISTRY, MEDICINAL | SERIES | CHEMISTRY, ORGANIC | 5-HT2C receptor agonists | DERIVATIVES | DISCOVERY | Serotonin 5-HT2 Receptor Agonists - therapeutic use | Pyrimidines - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Azepines - chemical synthesis | Rats | Male | Serotonin 5-HT2 Receptor Agonists - pharmacology | Pyrimidines - pharmacology | Pyrimidines - chemistry | Serotonin 5-HT2 Receptor Agonists - chemistry | Azepines - therapeutic use | Urinary Incontinence - drug therapy | Azepines - pharmacology | Animals | Azepines - chemistry | Pyrimidines - therapeutic use | Dogs | Molecular Structure | Disease Models, Animal
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19. Full Text Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6-tetrahydropyridines as 5-HT2C agonists
by Conway, Richard J and Valant, Celine and Christopoulos, Arthur and Robertson, Alan D and Capuano, Ben and Crosby, Ian T
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 04/2012, Volume 22, Issue 7, pp. 2560 - 2564
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1,2,3,6-tetrahydropyridines were synthesized and their biological activity at the 5-HT... 
Synthesis | Anti-obesity | 5-HT2C agonists | SAR | SITE | CHEMISTRY, MEDICINAL | CHLOROPHENYLPIPERAZINE | RECEPTOR AGONISTS | FOOD-INTAKE | CHEMISTRY, ORGANIC | ANTAGONISTS | Calcium - metabolism | Stereoisomerism | Appetite Depressants - pharmacology | Humans | Receptor, Serotonin, 5-HT2C - metabolism | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | Pyridines - chemical synthesis | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Piperidines - chemical synthesis | Serotonin Antagonists - pharmacology | Animals | Piperidines - pharmacology | Receptor, Serotonin, 5-HT2C - chemistry | Protein Binding | Appetite Depressants - chemical synthesis | Pyridines - pharmacology | Kinetics | Radioligand Assay | Ergolines - pharmacology | Structure-activity relationships | Serotonin S2 receptors
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20. Full Text Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT 2C Receptor Agonists
by Carpenter, Joseph and Wang, Ying and Wu, Gang and Feng, Jianxin and Ye, Xiang-Yang and Morales, Christian L and Broekema, Matthias and Rossi, Karen A and Miller, Keith J and Murphy, Brian J and Wu, Ginger and Malmstrom, Sarah E and Azzara, Anthony V and Sher, Philip M and Fevig, John M and Alt, Andrew and Bertekap, Jr, Robert L and Cullen, Mary Jane and Harper, Timothy M and Foster, Kimberly and Luk, Emily and Xiang, Qian and Grubb, Mary F and Robl, Jeffrey A and Wacker, Dean A
Journal of medicinal chemistry, 07/2017, Volume 60, Issue 14, p. 6166
Agonism of the 5-HT receptor represents one of the most well-studied and clinically proven mechanisms for pharmacological weight reduction. Selectivity over... 
Serotonin 5-HT2 Receptor Agonists - pharmacokinetics | Receptor, Serotonin, 5-HT2B - metabolism | Humans | Microsomes, Liver - metabolism | Receptor, Serotonin, 5-HT2C - metabolism | Cell Membrane Permeability | Male | Serotonin 5-HT2 Receptor Agonists - pharmacology | Structure-Activity Relationship | Flavones - chemistry | Arginine - analogs & derivatives | Brain - metabolism | Flavones - chemical synthesis | HEK293 Cells | Arginine - chemical synthesis | Flavones - pharmacology | Caco-2 Cells | Serotonin 5-HT2 Receptor Agonists - chemical synthesis | ATP Binding Cassette Transporter, Subfamily G, Member 2 - genetics | Membranes, Artificial | Rats, Sprague-Dawley | Serotonin 5-HT2 Receptor Agonists - chemistry | ATP Binding Cassette Transporter, Subfamily B, Member 1 - genetics | Arginine - chemistry | Feeding Behavior - drug effects | Mice, Knockout | Animals | Arginine - pharmacology | Receptor, Serotonin, 5-HT2C - genetics | Mutation | Receptor, Serotonin, 5-HT2A - metabolism
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