We tested several histamine H(1) receptor (H(1)R) and antagonists for their differences in agonists binding affinities between human and guinea pig H(1)Rs transiently expressed in African green monkey kidney (COS-7) cells. Especially, the bivalent agonist histaprodifen-histamine dimer (HP-HA) shows a higher affinity for guinea pig than for human H(1)Rs. Based on the structure of HP-HA, we have ...

GPRC6A is a Family C G protein-coupled receptor recently discovered and deorphanized by our group. This study integrates chemogenomic ligand inference, homology modeling, compound synthesis, and pharmacological mechanism-of-action studies to disclose two noticeable results of methodological and pharmacological character: (1) chemogenomic lead identification through the first, to our knowledge, ...

Despite there being a large body of work, the exact molecular details underlying ion selectivity and transport in the potassium channel have not been fully uncovered. One major reason has been the lack of experimental methods that can probe these mechanisms dynamically on their biologically relevant timescales. Recently, it was suggested that quantum coherence and its interplay with thermal vib...

Modeling of an esterification reaction in a batch pervaporation membrane reactor (PVMR), and an analysis of the PVMR performance under different reaction conditions for different membrane characteristics are presented. Esterification of ethyl alcohol with acetic acid was considered as the model reaction. The PVMR performance for this reaction could be represented by a 2-step series model. The P...

Novel 1-, 5-, and 8-substituted analogues of sumanirole (1), a dopamine D2/D3 receptor (D2R/D3R) agonist, were synthesized. Binding affinities at both D2R and D3R were higher when determined in competition with the agonist radioligand [(3)H]7-hydroxy-N,N-dipropyl-2-aminotetralin (7-OH-DPAT) than with the antagonist radioligand [(3)H]N-methylspiperone. Although 1 was confirmed as a D2R-preferent...

The activation of heteromeric and homomeric nicotinic acetylcholine receptors was studied in Xenopus laevis oocytes to identify key structures of putative agonist molecules associated with the selective activation of homomeric alpha7 receptors. We observed that selectivity between alpha7 and alpha4beta2 was more readily obtained than selectivity between alpha7 and alpha3beta4. Based on structur...

The direction selectivity of cortical neurons can be accounted for by asymmetric lateral connections. Such lateral connectivity leads to a network dynamics with characteristic properties that can be exploited for distinguishing in neurophysiological experiments this mechanism for direction selectivity from other possible mechanisms. We present a mathematical analysis for a class of direction-se...

The catalyst Pt-Ta supported on 7-alumina was prepared by impregnation with solution containing compoundsof II21K1.0. and Ta205 The Pt concentration was kept constant at 0.2 vet% while the concentration of thetantalum was 0,4 wt%. The activity and selectivity of catalyst were determined under conditions at 450-500 °Cand 15-30 atm.. with molar ratio H2/C[H,e5 and WH=1.5mL/h for converted n-hepta...

ch4, c2h6 and c2h4 are the most important outlet gaseous of oxidative couple methane (ocm) reaction and this process is a new technology for conversion of natural gas to ethane and ethylene products. in this study, adsorption of ocm outlet hydrocarbons over 10x zeolite has been examined at equilibrium conditions. temperature and pressure are the most effective operational parameters in the batc...

bimetallic pt-v supported by gamma-alumina is used to observe the changes of nheptanewhen passed over this catalyst. the pt concentration was kept constant at0.1wt% while the concentration of the vanadium was 0.5wt%. the activity andselectivity of catalyst have been determined under conditions at 450-500 degreescentigrade and 15-30 attn. the experimental results show that the addition of second...