Zobrazeno 1 - 10
of 21
pro vyhledávání: '"Lerisetron"'
Autor:
Fanuel Mebrahtu, Leslie J. Street, Marine Barnabe, Rudolf Mueller, Nina Lawrence, Matthias Rottmann, Virsinha Reddy, Aloysius T. Nchinda, Ravinder Reddy Kondreddi, Dale Taylor, Lloyd Tanner, Charles J. Eyermann, Kelly Chibale, Suresh B. Lakshminarayana, Bin Zou
Publikováno v:
ACS Omega
ACS Omega, Vol 5, Iss 12, Pp 6967-6982 (2020)
ACS Omega, Vol 5, Iss 12, Pp 6967-6982 (2020)
A phenotypic whole cell high-throughput screen against the asexual blood and liver stages of the malaria parasite identified a benzimidazole chemical series. Among the hits were the antiemetic benzimidazole drug Lerisetron 1 (IC50 NF54 = 0.81 μM) an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d63cce4b28ef53dc6673f59d7565d672
https://pubmed.ncbi.nlm.nih.gov/32258933
https://pubmed.ncbi.nlm.nih.gov/32258933
Autor:
Harish S. Parihar, Marvin K. Schulte, Karen S Kirschbaum, Prasad R. Joshi, Asha Suryanarayanan, Padma Venkataraman, Chun Ma
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2133-2136
The design, synthesis, and use of lerisetron-based molecular probes to investigate the 5-HT 3 R binding site are described. A SAR study, which involved distance and electronic parameter modifications of lerisetron's N -benzyl group, resulted in the d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5615777a50453712c970d470f927e786
https://doi.org/10.1016/s0960-894x(01)00417-6
https://doi.org/10.1016/s0960-894x(01)00417-6
Publikováno v:
Pharmaceutical Research. 18:838-845
Purpose. To examine the effect of changes in plasma α1-acid glycoprotein (AAG) levels on the pharmacokinetics (PK) and pharmacodynamics (PD) of lerisetron, a novel serotonin 5-HT3 receptor antagonist, in the rat.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::31900fbde03e425842e1a0fc5e9ea730
https://doi.org/10.1023/a:1011096714860
https://doi.org/10.1023/a:1011096714860
Publikováno v:
Acta Oncologica. 37:759-763
The 5-HT3 receptor antagonists are the most potent antiemetics known at present. Lerisetron is a new 5-HT3 receptor antagonist chemically unrelated to other antagonists like Ondansetron. An emesis model in the dog induced by irradiation with 60Co was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08b9c505ee565ce96c223f6a50932055
https://doi.org/10.1080/028418698430160
https://doi.org/10.1080/028418698430160
Publikováno v:
ChemInform. 28
A series of 2-piperazinylbenzimidazole derivatives were prepared and evaluated as 5-HT3 receptor antagonists. Their 5-HT3 receptor affinities were evaluated by radioligand binding assays, and their abilities to inhibit the 5-HT-induced Bezold−Jaris
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::bdd00c6b655c9301ebb3cb204dfcf490
https://doi.org/10.1002/chin.199722172
https://doi.org/10.1002/chin.199722172
Autor:
Ana Gonzalo, Maria Luisa Lucero, Aurelio Orjales, Leire de la Fuente, John C. Lukas, Fátima Ortega, Rosario Calvo, Antonio Quintana, Elena Suarez, Nerea Jauregizar
Publikováno v:
Pharmaceutical research. 22(11)
The twofold aim of this study was to characterize in vivo in rats the pharmacokinetics (PK) and pharmacodynamics (PD) of L6-OH, a metabolite of lerisetron with in vitro pharmacological activity, and evaluate the extent to which L6-OH contributes to t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d2d8b4bbe3cef75004efe3e55616284
https://pubmed.ncbi.nlm.nih.gov/16158214
https://pubmed.ncbi.nlm.nih.gov/16158214
Publikováno v:
Arzneimittel-Forschung. 52(9)
The purpose of these studies was to evaluate the effect of lerisetron (1-phenyl-methyl-2-piperazinyl-1H-benzimidazole hydrochloride, CAS 143257-98-1, F- 0930-RS2), a new 5-HT 3 receptor antagonist, on ipecacuanha-induced nausea and vomiting. The ipec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa55f7e690b34039a8ad9462eb1c25ac
https://pubmed.ncbi.nlm.nih.gov/12404884
https://pubmed.ncbi.nlm.nih.gov/12404884
Autor:
Ewa Raczka, Leire de la Fuente, Elena Suarez, Antonio Quintana, Rosario Calvo, Nerea Jauregizar
Publikováno v:
Gerontology. 49(4)
Background: The importance of studying the effects of age on the pharmacokinetics and pharmacodynamics of lerisetron – a new 5-hydroxytryptamine-3 (serotonin) receptor antagonist – comes from the facts that lerisetron will be administered to pati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4340d4e10c7d2ae008277236156a8409
https://pubmed.ncbi.nlm.nih.gov/12792155
https://pubmed.ncbi.nlm.nih.gov/12792155
Autor:
Elena Suarez, Ma Luisa Lucero, Ana Gonzalo, Ewa Raczka, Ignacio F. Trocóniz, Rosario Calvo, Aurelio Orjales, R.M. Jiménez
Publikováno v:
Cancer chemotherapy and pharmacology. 42(5)
The aim of this study was, (1) to characterize the serum protein binding of lerisetron, a new 5-hydroxytryptamine (5-HT3) receptor antagonist under investigation as an antiemetic agent, and (2) to measure the percentage of unbound lerisetron in cance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7c7a33ecda54f756c33e892c8b9616ee
https://pubmed.ncbi.nlm.nih.gov/9771958
https://pubmed.ncbi.nlm.nih.gov/9771958
Autor:
Karen S Kirschbaum, Marvin K. Schulte, Padmavati Venkataraman, Harish S. Parihar, Srinivasan P Venkatachalan, Prasad R. Joshi, Mani Muthalagi
Publikováno v:
BMC Biochemistry. 3:16
Background Lerisetron, a competitive serotonin type 3 receptor (5-HT3R) antagonist, contains five functional groups capable of interacting with amino acids in the 5-HT3R binding site. Site directed mutagenesis studies of the 5-HT3AR have revealed sev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4b92125113dd5d951fc5e3c728f89760
https://doi.org/10.1186/1471-2091-3-16
https://doi.org/10.1186/1471-2091-3-16