Literature

Robert B. Kargbo − Usona Institute, San Luis Obispo,
California 93401-7337, United States; 3-(2-(Aminoethyl)-indol-4-ol Derivatives, Methods of
Preparation Thereof, and the Use as 5-HT2 Receptor
Modulators

Zhang G, McCorvy JD, Shen S, Cheng J, Roth BL, Kozikowski AP. Design of fluorinated cyclopropane derivatives of 2-phenylcyclopropylmethylamine leading to identification of a selective serotonin 2C (5-HT) receptor agonist without 5-HT agonism. European Journal of Medicinal Chemistry.2019. 182: 111626. PMID 31445232 DOI: 10.1016/j.ejmech.2019.111626

Zhang G, Cheng J, McCorvy JD, Lorello PJ, Caldarone BJ, Roth BL, Kozikowski AP. Discovery of N-Substituted 2-Phenylcyclopropylmethylamines as Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists for Potential Use as Antipsychotic Medications. Journal of Medicinal Chemistry. 2017. PMID 28657744 DOI: 10.1021/acs.jmedchem.7b00584

Pogorelov VM, Rodriguiz RM, Cheng J, Huang M, Schmerberg CM, Meltzer HY, Roth BL, Kozikowski AP, Wetsel WC. 5-HT2C Agonists Modulate Schizophrenia-Like Behaviors in Mice. Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology. 2017. PMID 28294132 DOI: 10.1038/npp.2017.52

Cheng J, McCorvy JD, Giguère PM, Zhu H, Kenakin T, Roth BL, Kozikowski AP. Design and Discovery of Functionally Selective Serotonin 2C (5-HT2C) Receptor Agonists. Journal of Medicinal Chemistry. 2016. PMID 27726356 DOI: 10.1021/acs.jmedchem.6b01194

Onajole OK, Vallerini GP, Eaton JB, Lukas RJ, Brunner D, Caldarone BJ, Kozikowski AP. Synthesis and Behavioral Studies of Chiral Cyclopropanes as Selective α4β2-Nicotinic Acetylcholine Receptor Partial Agonists Exhibiting an Antidepressant Profile. Part III. Acs Chemical Neuroscience. 2016. PMID 27035276 DOI: 10.1021/acschemneuro.6b00050

Cheng J, Giguère PM, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Huang XP, Zhu H, McCorvy JD, Wetsel WC, Roth BL, Kozikowski AP. Further Advances in Optimizing (2-Phenylcyclopropyl)methylamines as Novel Serotonin 2C Agonists: Effects on Hyperlocomotion, Prepulse Inhibition, and Cognition Models. Journal of Medicinal Chemistry. 2015. PMID 26704965 DOI: 10.1021/acs.jmedchem.5b01153

Cheng J, Kozikowski AP. We Need 2C but Not 2B: Developing Serotonin 2C (5-HT2C ) Receptor Agonists for the Treatment of CNS Disorders. Chemmedchem. 2015. PMID 26507582 DOI: 10.1002/cmdc.201500437

Cheng J, Giguère PM, Onajole OK, Lv W, Gaisin A, Gunosewoyo H, Schmerberg CM, Pogorelov VM, Rodriguiz RM, Vistoli G, Wetsel WC, Roth BL, Kozikowski AP. Optimization of 2-phenylcyclopropylmethylamines as selective serotonin 2C receptor agonists and their evaluation as potential antipsychotic agents. Journal of Medicinal Chemistry. 2015. 58: 1992-2002. PMID 25633969 DOI: 10.1021/jm5019274

Zhang HK, Yu LF, Eaton JB, Whiteaker P, Onajole OK, Hanania T, Brunner D, Lukas RJ, Kozikowski AP. Chemistry, pharmacology, and behavioral studies identify chiral cyclopropanes as selective α4β2 -nicotinic acetylcholine receptor partial agonists exhibiting an antidepressant profile. Part II. Journal of Medicinal Chemistry. 2013. 56: 5495-504. PMID 23734673 DOI: 10.1021/jm400510u

Chen G, Cho SJ, Huang XP, Jensen NH, Svennebring A, Sassano MF, Roth BL, Kozikowski AP. Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity. Acs Medicinal Chemistry Letters. 2011. 2: 929-932. PMID 22778800 DOI: 10.1021/ml200206z

Kozikowski AP, Cho SJ, Jensen NH, Allen JA, Svennebring AM, Roth BL. HTS and rational drug design to generate a class of 5-HT(2C)-selective ligands for possible use in schizophrenia. Chemmedchem. 2010. 5: 1221-5. PMID 20533502 DOI: 10.1002/cmdc.201000186

Cho SJ, Jensen NH, Kurome T, Kadari S, Manzano ML, Malberg JE, Caldarone B, Roth BL, Kozikowski AP. Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action. Journal of Medicinal Chemistry. 2009. 52: 1885-902. PMID 19284718 DOI: 10.1021/jm801354e

Kozikowski AP, Zhao L, Zhang A, Wang CZ, Flippen-Anderson J, Johnson KM. Structural remodeling of cocaine: design and synthesis of trisubstituted cyclopropanes as selective serotonin reuptake inhibitors. Chemmedchem. 2006. 1: 58-65. PMID 16892336 DOI: 10.1002/cmdc.200500016

McCorvy JD and Roth, BL. Structure and function of G protein-coupled receptors. Pharmacology & Therapeutics. 2015. 150:129-42. PMCID: PMC4414735 DOI: 10.1016/j.pharmthera.2015.01.009

Tan L, Yan W, McCorvy JD, Cheng J. Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. J Med Chem 2018. 61(22):9841-9878. PMID: 29939744 DOI: 10.1021/acs.jmedchem.8b00435

McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RHJ, Che T, Jin J, Roth BL. Structural determinants of 5-HT 2B receptor activation and biased agonism. Nature Struct Mol Bio. 2018. 25(9):787-796. PMID: 30127358 DOI: 10.1038/s41594-018-0116-7

Wacker D, Wang S, McCorvy JD, Betz RM, Venkatakrishnan, Levit A, Lansu K, Schools Z, Che T, Nichols DE, Shoichet BK, Dror RO, Roth BL. Structure of LSD bound to a human serotonin receptor. Cell 2017. 168(3):377-389 PMCID:PMC5289311 DOI: 10.1016/j.cell.2016.12.033

Peng Y, McCorvy JD, Harpsøe K, Lansu K, Yuan S, Popov P, Qu L, Pu M, Che T, Nikolajsen LF, Huang XP, Wu Y, Shen L, Bjørn-Yoshimoto WE, Ding K, Wacker D, Han GW, Cheng JJ, Katritch V, Jensen AA, Hanson MA, Zhao S, Gloriam DE, Roth BL, Stevens RC, Liu ZJ. Structures of the 5-HT2C receptor illuminate the structural basis of GPCR polypharmacology. Cell 2018. 172(4):719-730. PMID: 29398112 DOI: 10.1016/j.cell.2018.01.001