60703-69-7Relevant articles and documents
Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH 1R, but low affinity to hH4R
Wagner, Eva,Wittmann, Hans-Joachim,Elz, Sigurd,Strasser, Andrea
, p. 6274 - 6280 (2011/11/29)
In literature, a synergism between histamine H1 and H 4 receptor is discussed. Furthermore, it was shown, that the combined application of mepyramine, a H1 antagonist and JNJ7777120, a H 4 receptor ligand leads to a synergistic effect in the acute murine asthma model. Thus, the aim of this study was to develop new hybrid ligands, containing one H1 and one H4 pharmacophor, connected by an appropriate spacer, in order to address both, H1R and H 4R. Within this study, we synthesized nine hybrid compounds, which were pharmacologically characterized at hH1R and hH4R. The new compounds revealed (high) affinity to hH1R, but showed only low affinity to hH4R. Additionally, we performed molecular dynamic studies for some selected compounds at hH1R, in order to obtain information about the binding mode of these compounds on molecular level.
CYCLIC ETHER COMPOUNDS AS SODIUM CHANNEL MODULATORS
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, (2008/06/13)
A compound of the formula: wherein R 1 and R 2 each represents hydrogen, lower alkyl which may be substituted or acyl; R 3, R 4 and R 5 each represents lower alkyl which may be substituted or lower alkoxy which may be substituted or R 4 and R 5 taken together represent a 5-or 6-membered carbocyclic group; R 6 represents lower alkyl; Ar represents an aromatic group which may be substituted; ring A represents a 5-to 8-membered nitrogen-containing heterocyclic ring which may be substituted; X represents lower alkylene which may be substituted; Y represents carbon or nitrogen; Za represents CH 2, COCH 2, OCH 2, SCH 2, NHCH 2, etc.; Zb represents a bond or a divalent aliphatic hydrocarbon group which may be substituted and may contain O, N or S; and m represents an integer of 1 to 3, or a salt thereof is useful for a pharmaceutical composition for modulating sodium channel.
Development of novel, potent, and selective dopamine reuptake inhibitors through alteration of the piperazine ring of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines (GBR 12935 and GBR 12909)
Matecka, Dorota,Rothman, Richard B.,Radesca, Lilian,De Costa, Brian R.,Dersch, Christina M.,Partilla, John S.,Pert, Agu,Glowa, John R.,Wojnicki, Francis H. E.,Rice, Kenner C.
, p. 4704 - 4716 (2007/10/03)
The design, synthesis, and biological evaluation of compounds related to the dopamine (DA) uptake inhibitors: 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)piperazine (1) and 1-[2-[bis-(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (2) (GBR