L
Laykea Tafesse
Researcher at Purdue Pharma
Publications - 91
Citations - 1646
Laykea Tafesse is an academic researcher from Purdue Pharma. The author has contributed to research in topics: Parkinsonism & Piperidine. The author has an hindex of 19, co-authored 91 publications receiving 1607 citations.
Papers
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Journal ArticleDOI
Pharmacological and pharmacokinetic characterization of the cannabinoid receptor 2 agonist, GW405833, utilizing rodent models of acute and chronic pain, anxiety, ataxia and catalepsy.
Kenneth J. Valenzano,Laykea Tafesse,Gary Lee,James E. Harrison,Jamie Boulet,Susan L. Gottshall,Lilly Mark,Michelle S. Pearson,Wendy S. Miller,Shen Shan,Leyana Rabadi,Yakov Rotshteyn,Suzanne M. Chaffer,Paul I. Turchin,David A. Elsemore,Mathew Toth,Lee Koetzner,Garth Whiteside +17 more
TL;DR: Data support the tenet that selective CB2 receptor agonists have the potential to treat pain without eliciting the centrally-mediated side effects associated with non-selective cannabinoid agonists, and highlight the utility of GW405833 for the investigation of CB2 physiology.
Journal ArticleDOI
N-(4-Tertiarybutylphenyl)-4-(3-chloropyridin-2-yl)tetrahydropyrazine -1(2H)-carbox-amide (BCTC), a Novel, Orally Effective Vanilloid Receptor 1 Antagonist with Analgesic Properties: I. In Vitro Characterization and Pharmacokinetic Properties
Kenneth J. Valenzano,Elfrida R. Grant,Gang Wu,Mohamed Hachicha,Lori Schmid,Laykea Tafesse,Qun Sun,Yakov Rotshteyn,Joseph Francis,James T. Limberis,Shiazah Malik,Edward R. Whittemore,D. Dianne Hodges +12 more
TL;DR: In vitro pharmacology of a high potency, selective VR1 antagonist that, unlike capsazepine, has potent blocking effects on low pH-induced activation of rat VR1 is described, making it a more suitable candidate for testing the role played by VR1 in rat models of human disease.
Patent
Therapeutic agents useful for treating pain
TL;DR: In this paper, a 4-Tetrazolyl-4-phenylpiperidine (4-TTE)-compound was used for treating or preventing pain or diarrhea in an animal.
Journal ArticleDOI
4-(2-pyridyl)piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists.
Qun Sun,Laykea Tafesse,Khondaker Islam,Xiaoming Zhou,Sam Victory,Chongwu Zhang,Mohamed Hachicha,Lori Schmid,Aniket Patel,Yakov Rotshteyn,Kenneth J. Valenzano,Donald J. Kyle +11 more
TL;DR: A series of 4-(2-pyridyl)piperazine-1-carboxamide analogues based on the lead compound 1 was synthesized and evaluated for VR1 antagonist activity in capsaicin-induced (CAP) and pH (5.5)-induced (pH) FLIPR assays in a rat VR1-expressing HEK293 cell line.
Journal ArticleDOI
Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists
Laykea Tafesse,Qun Sun,Lori Schmid,Kenneth J. Valenzano,Yakov Rotshteyn,Xin Su,Donald J. Kyle +6 more
TL;DR: A structurally biased chemical library of pyridazinylpiperazine analogs was prepared in an effort to improve the pharmaceutical and pharmacological profile of the lead compound N-(4-tertiarybutylphenyl)-4-chloropyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide (BCTC).