Search Results - "Koblan, Kenneth S."

A Non–D2-Receptor-Binding Drug for the Treatment of Schizophrenia by Koblan, Kenneth S, Kent, Justine, Hopkins, Seth C, Krystal, John H, Cheng, Hailong, Goldman, Robert, Loebel, Antony

“…In a randomized trial involving schizophrenic patients with acute psychosis, a new oral drug that does not have a dopamine D2-receptor–binding mechanism of…”
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Effect of TAAR1/5-HT1A agonist SEP-363856 on REM sleep in humans by Hopkins, Seth C., Dedic, Nina, Koblan, Kenneth S.

“…SEP-363856 is a trace amine-associated receptor 1 (TAAR1) and 5-hydroxytryptamine type 1A (5-HT 1A ) agonist, currently in Phase 3 clinical trials for the…”
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Population pharmacokinetic analysis of ulotaront in subjects with schizophrenia by Galluppi, Gerald R., Polhamus, Daniel G., Fisher, Jeannine M., Hopkins, Seth C., Koblan, Kenneth S.

“…Ulotaront (SEP‐363856) is a trace amine–associated receptor 1 agonist with 5‐HT1A agonist activity in phase III development for the treatment of schizophrenia…”
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TAAR1 agonists improve glycemic control, reduce body weight and modulate neurocircuits governing energy balance and feeding by Dedic, Nina, Wang, Lien, Hajos-Korcsok, Eva, Hecksher-Sørensen, Jacob, Roostalu, Urmas, Vickers, Steven P., Wu, Serena, Anacker, Christoph, Synan, Colleen, Jones, Philip G., Milanovic, Snezana, Hopkins, Seth C., Bristow, Linda J., Koblan, Kenneth S.

“…Metabolic Syndrome, which can be induced or exacerbated by current antipsychotic drugs (APDs), is highly prevalent in schizophrenia patients. Recent…”
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Comparative Bioequivalence of Tablet and Capsule Formulations of Ulotaront and the Effect of Food on the Pharmacokinetics of the Tablet Form in Humans by Chen, Yu-Luan, Tsukada, Hironobu, Milanovic, Snezana, Shi, Lei, Li, Yan, Mao, Yongcai, Koblan, Kenneth S., Galluppi, Gerald R.

“…Introduction Ulotaront (SEP-363856), a dual trace animeassociated receptor 1 (TAAR1) and 5-HT 1A receptor agonist, is in phase 3 clinical development for the…”
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Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine by Salvatore, Christopher A, Hershey, James C, Corcoran, Halea A, Fay, John F, Johnston, Victor K, Moore, Eric L, Mosser, Scott D, Burgey, Christopher S, Paone, Daniel V, Shaw, Anthony W, Graham, Samuel L, Vacca, Joseph P, Williams, Theresa M, Koblan, Kenneth S, Kane, Stefanie A

“…Calcitonin gene-related peptide (CGRP) is a potent neuropeptide that plays a key role in the pathophysiology of migraine headache. CGRP levels in the cranial…”
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Potent, Orally Bioavailable Calcitonin Gene-Related Peptide Receptor Antagonists for the Treatment of Migraine:  Discovery of N-[(3R,6S)-6-(2,3-Difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974) by Paone, Daniel V, Shaw, Anthony W, Nguyen, Diem N, Burgey, Christopher S, Deng, James Z, Kane, Stefanie A, Koblan, Kenneth S, Salvatore, Christopher A, Mosser, Scott D, Johnston, Victor K, Wong, Bradley K, Miller-Stein, Cynthia M, Hershey, James C, Graham, Samuel L, Vacca, Joseph P, Williams, Theresa M

“…Calcitonin gene-related peptide (CGRP) has been implicated in the pathogenesis of migraine. Herein we describe optimization of CGRP receptor antagonists based…”
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Effects of ulotaront on brain circuits of reward, working memory, and emotion processing in healthy volunteers with high or low schizotypy by Perini, Francesca, Nazimek, Jadwiga Maria, Mckie, Shane, Capitão, Liliana P., Scaife, Jessica, Pal, Deepa, Browning, Michael, Dawson, Gerard R., Nishikawa, Hiroyuki, Campbell, Una, Hopkins, Seth C., Loebel, Antony, Elliott, Rebecca, Harmer, Catherine J., Deakin, Bill, Koblan, Kenneth S.

“…Ulotaront, a trace amine-associated receptor 1 (TAAR1) and serotonin 5-HT1A receptor agonist without antagonist activity at dopamine D 2 or the serotonin…”
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Orexin receptor antagonism prevents transcriptional and behavioral plasticity resulting from stimulant exposure by Winrow, Christopher J., Tanis, Keith Q., Reiss, Duane R., Rigby, Alison M., Uslaner, Jason M., Uebele, Victor N., Doran, Scott M., Fox, Steven V., Garson, Susan L., Gotter, Anthony L., Levine, David M., Roecker, Anthony J., Coleman, Paul J., Koblan, Kenneth S., Renger, John J.

“…Orexin is a key neurotransmitter of central arousal and reward circuits in the CNS. Two receptors respond to orexin signaling, Orexin 1 Receptor (OX1R) and…”
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Challenges in the clinical development of non-D2 compounds for schizophrenia by Hopkins, Seth C., Lew, Robert, Zeni, Courtney, Koblan, Kenneth S.

“…Schizophrenia is a chronic, heterogeneous, severe psychiatric disorder characterized by a spectrum of symptomology and is associated with substantial morbidity…”
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Receptor Activity-modifying Protein 1 Determines the Species Selectivity of Non-peptide CGRP Receptor Antagonists by Mallee, John J, Salvatore, Christopher A, LeBourdelles, Beatrice, Oliver, Kevin R, Longmore, Jenny, Koblan, Kenneth S, Kane, Stefanie A

“…The heterodimeric CGRP receptor requires co-expression of calcitonin receptor-like receptor (CRLR) and an accessory protein called receptor activity-modifying…”
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LRRTM3 Promotes Processing of Amyloid-Precursor Protein by BACE1 and Is a Positional Candidate Gene for Late-Onset Alzheimer's Disease by Majercak, John, Ray, William J., Espeseth, Amy, Simon, Adam, Shi, Xiao-Ping, Wolffe, Carrie, Getty, Krista, Marine, Shane, Stec, Erica, Ferrer, Marc, Strulovici, Berta, Bartz, Steven, Gates, Adam, Xu, Min, Huang, Qian, Ma, Lei, Shughrue, Paul, Burchard, Julja, Colussi, Dennis, Pietrak, Beth, Kahana, Jason, Beher, Dirk, Rosahl, Thomas, Shearman, Mark, Hazuda, Daria, Sachs, Alan B., Koblan, Kenneth S., Seabrook, Guy R., Stone, David J.

“…Rare familial forms of Alzheimer's disease (AD) are thought to be caused by elevated proteolytic production of the Aβ42 peptide from the β-amyloid-precursor…”
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SEP-363856, a Novel Psychotropic Agent with a Unique, Non-D 2 Receptor Mechanism of Action by Dedic, Nina, Jones, Philip G, Hopkins, Seth C, Lew, Robert, Shao, Liming, Campbell, John E, Spear, Kerry L, Large, Thomas H, Campbell, Una C, Hanania, Taleen, Leahy, Emer, Koblan, Kenneth S

“…For the past 50 years, the clinical efficacy of antipsychotic medications has relied on blockade of dopamine D receptors. Drug development of non-D compounds,…”
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Discovery of a Potent, CNS‐Penetrant Orexin Receptor Antagonist Based on an N,N‐Disubstituted‐1,4‐diazepane Scaffold that Promotes Sleep in Rats by Whitman, David B., Cox, Christopher D., Breslin, Michael J., Brashear, Karen M., Schreier, John D., Bogusky, Michael J., Bednar, Rodney A., Lemaire, Wei, Bruno, Joseph G., Hartman, George D., Reiss , Duane R., Harrell, C. Meacham, Kraus, Richard L., Li, Yuxing, Garson, Susan L., Doran, Scott M., Prueksaritanont, Thomayant, Li, Chunze, Winrow, Christopher J., Koblan, Kenneth S., Renger, John J., Coleman, Paul J.

“…Silent Night: Antagonism of the orexin (or hypocretin) system has recently been identified as a novel mechanism for the treatment of insomnia. Herein, we…”
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A Randomized, Double-blind, Placebo-controlled Proof-of-Concept Trial to Evaluate the Efficacy and Safety of Non-racemic Amisulpride (SEP-4199) for the Treatment of Bipolar I Depression by Loebel, Antony, Koblan, Kenneth S., Tsai, Joyce, Deng, Ling, Fava, Maurizio, Kent, Justine, Hopkins, Seth C.

“…•Atypical antipsychotics with antagonist activity at the 5-HT7 receptor have been found to have antidepressant efficacy.•Amisulpride is a racemic (50:50)…”
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Discovery of Nonracemic Amisulpride to Maximize Benefit/Risk of 5‐HT7 and D2 Receptor Antagonism for the Treatment of Mood Disorders by Hopkins, Seth C., Wilkinson, Scott, Corriveau, Taryn J., Nishikawa, Hiroyuki, Nakamichi, Keiko, Loebel, Antony, Koblan, Kenneth S.

“…In contrast to the dose‐occupancy relationship in the treatment of schizophrenia, the minimal effective level of dopamine receptor 2 (D2R) blockade for…”
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TAAR1 and 5-HT1B receptor agonists attenuate autism-like irritability and aggression in rats prenatally exposed to valproic acid by Wang, Lien, Clark, Erin A., Hanratty, Lynsey, Koblan, Kenneth S., Foley, Andrew, Dedic, Nina, Bristow, Linda J.

“…Despite the rising prevalence of autism spectrum disorder (ASD), there remains a significant unmet need for pharmacotherapies addressing its core and…”
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Functional and pharmacological properties of canine ERG potassium channels by Wang, Jixin, Della Penna, Kimberly, Wang, Hao, Karczewski, Jerzy, Connolly, Thomas M, Koblan, Kenneth S, Bennett, Paul B, Salata, Joseph J

“…We established HEK-293 cell lines that stably express functional canine ether-à-go-go-related gene (cERG) K(+) channels and examined their biophysical and…”
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In Vitro ADME and Preclinical Pharmacokinetics of Ulotaront, a TAAR1/5-HT1A Receptor Agonist for the Treatment of Schizophrenia by Xiao, Guangqing, Chen, Yu-Luan, Dedic, Nina, Xie, Linghong, Koblan, Kenneth S., Galluppi, Gerald R.

“…Purpose Ulotaront (SEP-363856) is a TAAR1 agonist with 5-HT 1A agonist activity currently in clinical development for the treatment of schizophrenia. The…”
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Uncovering the genetic landscape for multiple sleep-wake traits by Winrow, Christopher J, Williams, Deanna L, Kasarskis, Andrew, Millstein, Joshua, Laposky, Aaron D, Yang, He S, Mrazek, Karrie, Zhou, Lili, Owens, Joseph R, Radzicki, Daniel, Preuss, Fabian, Schadt, Eric E, Shimomura, Kazuhiro, Vitaterna, Martha H, Zhang, Chunsheng, Koblan, Kenneth S, Renger, John J, Turek, Fred W

“…Despite decades of research in defining sleep-wake properties in mammals, little is known about the nature or identity of genes that regulate sleep, a…”
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