Výsledky vyhledávání - "B L, Trivedi"

Synthesis and 5-HT-3 Receptor Binding of 2- and 3-(Halo)alkoxyl Substituted (S)-N-(1-Azabicyclo [2.2.2]oct-3-yl)-5-chlorobenzamides as Potential Radioligands

Autor: Dennis E. Schmidt, Michael H. Ebert, B. L. Trivedi, Tomas de Paulis, William A. Hewlett, N. Scott Mason

Publikováno v: Nuclear Medicine and Biology. 25:141-153

In an effort to develop selective, high-affinity radioligands for the 5-HT-3 receptor, a series of homologues of 5-chloro-2,3-dimethoxy- N -(1-azabicyclo[2.2.2]oct-3-yl)benzamide (2b) was prepared in which individual methoxy groups were replaced by e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0d23c05fdd2132eabc4b1997e6ded943
https://doi.org/10.1016/s0969-8051(97)00161-3

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Synthesis and 5-HT-3 receptor binding activity of 5-[125I]iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide and its 5-halogen-2-alkoxyl homologues

Autor: B. L. Trivedi, T. De Paulis, William A. Hewlett, Dennis E. Schmidt, Michael H. Ebert, N. S. Mason

Publikováno v: European Journal of Medicinal Chemistry. 32:385-396

Summary ( S )-5-Iodo-2,3-dimethoxy- N -(1-azabicyclo[2.2.2]oct-3-yl)benzamide (MIZAC) was prepared from 5-iodo-2,3-dimethoxybenzoyl chloride and ( S )-3-aminoquinuclidine. [ 125 I]Iodode-stannylation of its corresponding 5-tri- n -butyltin derivative

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7631ac34a863824971cf57a5aeddcf03
https://doi.org/10.1016/s0223-5234(97)81676-5

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Synthesis and Radiolabeling of (S)-4-Amino-5-iodo-2-methoxy-N-(1-azabicyclo(2.2.2)oct-3-yl)benzamide, the Active Enantiomer of (125I)Iodozacopride, and Re-evaluation of Its 5-HT3 Receptor Affinity

Autor: B. L. Trivedi, Tomas de Paulis, Michael H. Ebert, William A. Hewlett, Dennis E. Schmidt, Zhang-Jin Zhang, N. Scott Mason

Publikováno v: Chemical and Pharmaceutical Bulletin. 45:2079-2084

We report an improved synthesis of unlabeled (S)-iodozacopride, the radiolabeling of (S)-[125I]iodozacopride via deschloro-(S)-zacopride, and a re-evaluation of its affinity for the 5-HT3 receptor. Unlabeled (S)-iodozacopride was prepared in seven st

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e51d3f49b5d97d11781a74e842993ea4
https://doi.org/10.1248/cpb.45.2079

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(S)-4-amino-5-chloro-3-iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (TRIZAC), a high-affinity ligand for the 5-HT-3 receptor

Autor: B. L. Trivedi, William A. Hewlett, Dennis E. Schmidt, Michael H. Ebert, Tomas de Paulis, Zhang-Jin Zhang

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:2657-2662

TRIZAC is one of the most potent 5-HT-3 receptor antagonist reported to date, having 20-fold higher affinity than (S)-5-todozacopride. This high affinity (K1 0.05 ± 0.01 nM) and a moderate apparent lipophilicity (log Papp 2.12) makes TRIZAC a promis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::aaf0d6b2a60d313289f6b6244bda0023
https://doi.org/10.1016/s0960-894x(96)00497-0

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Dual blockade of the EGFR and COX-2 pathways: A phase II trial of cetuximab and celecoxib in patients with chemotherapy refractory metastatic colorectal cancer

Autor: Albert C. Lockhart, B. L. Trivedi, Nipun B. Merchant, Bonnie LaFleur, Jordan Berlin, Emily Chan, Christine H. Chung, Mace L. Rothenberg, Robert J. Coffey

The epidermal growth factor receptor (EGFR) and cyclooxygenase-2 (COX-2) pathways play key and often complementary roles in the pathogenesis of colorectal cancer (CRC). This study explores the clinical and biological effects of combined blockade of t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f10ae120fc2dd233bd38351a4e1624c1
https://europepmc.org/articles/PMC3133812/

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ChemInform Abstract: Synthesis and 5-HT-3 Receptor Binding Activity of 5-(125I)Iodo-2,3- dimethoxy-N-(1-azabicyclo(2.2.2)oct-3-yl)benzamide and Its 5-Halogen-2- alkoxyl Homologues

Autor: T. De Paulis, B. L. Trivedi, Dennis E. Schmidt, N. S. Mason, William A. Hewlett, Michael H. Ebert

Publikováno v: ChemInform. 28

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::960636caae55561fcf34f1834411d19a
https://doi.org/10.1002/chin.199743273

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Ligand-dependent activation of the epidermal growth factor receptor by secondary bile acids in polarizing colon cancer cells

Autor: Nipun B. Merchant, B. L. Trivedi, Robert J. Coffey, Christopher M. Rogers, Jason D. Morrow

Publikováno v: Surgery. 138(3)

Secondary bile acids such as deoxycholic acid (DCA) are known to promote colorectal cancer (CRC). Increasing evidence suggests that DCA-induced signaling is mediated by activation of the epidermal growth factor receptor (EGFR). We have shown that act

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::62df8936c566c26f79a594bde696c216
https://pubmed.ncbi.nlm.nih.gov/16213893

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Anxiolytic-like effects of DAIZAC, a selective high-affinity 5-HT(3) receptor antagonist, in the mouse elevated plus-maze

Autor: B. L. Trivedi, Dennis E. Schmidt, William A. Hewlett, Zhang-Jin Zhang, Tomas de Paulis, Michael H. Ebert, Emmanuel S. Onaivi

Publikováno v: Pharmacology, biochemistry, and behavior. 69(3-4)

Behavioral effects of desamino-3-iodozacopride (DAIZAC) [(S)-5-chloro-3-iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide], a selective high-affinity 5-HT(3) receptor antagonist (K(D) 0.14 nM), were evaluated in the mouse elevated plus-maze usi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7099304f530c2190f537decef38eeeb0
https://pubmed.ncbi.nlm.nih.gov/11509218

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