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001-es BibID:	BIBFORM020696
Első szerző:	Choi, Hyun-Kyung
Cím:	Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists / Choi Hyun-Kyung, Choi Sun, Lee Yoonji, Kang Dong Wook, Ryu HyungChul, Maeng Han-Joo, Chung Suk-Jae, Pavlyukovets Vladimir A., Pearce Larry V., Toth Attila, Tran Richard, Wang Yun, Morgan Matthew A., Blumberg Peter M., Lee Jeewoo
Dátum:	2009
ISSN:	0968-0896
Megjegyzések:	A series of non-vanillyl resiniferatoxin analogues, having 4-methylsulfonylaminophenyl and fluorophenyl moieties as vanillyl surrogates, have been investigated as ligands for rat TRPV1 heterologously expressed in Chinese hamster ovary cells. Although lacking the metabolically problematic 4-hydroxy substituent on the A-region phenyl ring, the compounds retained substantial agonist potency. Indeed, the 3-methoxy-4-methylsulfonylaminophenyl analog (1) was modestly (2.5-fold) more potent than RTX, with an EC(50)=0.106 nM. Further, it resembled RTX in its kinetics and pattern of stimulation of the levels of intracellular calcium in individual cells, as revealed by imaging. Compound 1 displayed modestly enhanced in vitro stability in rat liver microsomes and in plasma, suggesting that it might be a pharmacokinetically more favorable surrogate of resiniferatoxin. Molecular modeling analyses with selected analogues provide evidence that the conformational differences could affect their binding affinities, especially for the ester versus amide at the B-region.
Tárgyszavak:	Orvostudományok Klinikai orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:	Bioorganic & Medicinal Chemistry. - 17 : 2 (2009), p. 690-698. -
További szerzők:	Choi, Sun Lee, Yoonji Kang, Dong Wook Ryu, HyungChul Maeng, Han-Joo Chung, Suk-Jae Pavlyukovets, Vladimir A. Pearce, Larry V. Tóth Attila (1971-) (biológus) Tran, Richard Wang, Yun Morgan, Matthew A. Blumberg, Peter M. Lee, Jeewoo
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001-es BibID:	BIBFORM003725
Első szerző:	Chung, Jae-Uk
Cím:	Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists / Chung, J. U., Kim, S. Y., Lim, J. O., Choi, H. K., Kang, S. U., Yoon, H. S., Ryu, H., Kang, D. W., Lee, J., Kang, B., Choi, S., Toth, A., Pearce, L. V., Pavlyukovets, V. A., Lundberg, D. J., Blumberg, P. M.
Dátum:	2007
Megjegyzések:	A series of alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. alpha-Methyl substituted analogues showed potent and stereospecific antagonism to the action of capsaicin on rat TRPV1 heterologously expressed in Chinese hamster ovary cells. In particular, compounds 14 and 18, which possess the R-configuration, exhibited excellent potencies (respectively, K(i)=41 and 39.2 nM and K(i(ant))=4.5 and 37 nM)
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban Animals antagonists &amp Calcium Capsaicin Cells,Cultured chemical synthesis chemistry Cho Cells Cricetinae Cricetulus inhibitors metabolism Models,Molecular Molecular Structure pharmacology Rats Stereoisomerism Structure-Activity Relationship Thiourea TRPV Cation Channels
Megjelenés:	Bioorganic and Medical Chemistry. - 15 : 18 (2007), p. 6043-6053. -
További szerzők:	Kim, Su Yeon Lim, Ju-Ok Choi, Hyun-Kyung Kang, Sang-Uk Yoon, Hae-Seok Ryu, HyungChul Kang, Dong Wook Lee, Jeewoo Kang, Bomi Choi, Sun Tóth Attila (1971-) (biológus) Pearce, Larry V. Pavlyukovets, Vladimir A. Lundberg, Daniel J. Blumberg, Peter M.
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