Zobrazeno 1 - 10
of 36
pro vyhledávání: '"S R, Childers"'
Publikováno v:
Biochemical pharmacology. 62(4)
The efficacy of heroin metabolites for the stimulation of mu opioid receptor-mediated G-protein activation was investigated using agonist-stimulated [(35)S]guanosine-5'-O-(gamma-thio)-triphosphate binding. In rat thalamic membranes, heroin and its pr
Autor:
H M, Davies, V, Gilliatt, L A, Kuhn, E, Saikali, P, Ren, P S, Hammond, T, Sexton, S R, Childers
Publikováno v:
Journal of medicinal chemistry. 44(10)
A series of 3beta-naphthyltropane derivatives were synthesized and found to show high affinity at both the dopamine and serotonin transporter sites, leading to some of the most potent inhibitors known based on the tropane structure. Comparative molec
Publikováno v:
Bioorganicmedicinal chemistry letters. 11(4)
3Beta-(5-indolyl)-8-azabicyclo[3.2.1]octanes display potent binding affinity for both the dopamine and serotonin transporters, while certain 3beta-(4-(2-pyrrolyl)phenyl)-8-azabicyclo[3.2.1]octanes selectively bind to the serotonin transporter.
Autor:
C S, Breivogel, S R, Childers
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 295(1)
To investigate differences in agonist affinity, potency, and efficacy across rat brain regions, five representative cannabinoid compounds were investigated in membranes from three different rat brain regions for their ability to maximally stimulate [
Autor:
R H, Mach, M A, Nader, R L, Ehrenkaufer, H D, Gage, S R, Childers, L M, Hodges, M M, Hodges, H M, Davies
Publikováno v:
Synapse (New York, N.Y.). 37(2)
A series of PET imaging studies were conducted with two fluorine-18-labeled tropane analoges, [(18)F](+)-FTT and [(18)F](+)-FCT. Both compounds possessed a high affinity and selectivity for the dopamine transporter and had a higher accumulation in th
Autor:
S R, Letchworth, H R, Smith, L J, Porrino, B A, Bennett, H M, Davies, T, Sexton, S R, Childers
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 293(2)
PTT (2beta-propanoyl-3beta-[4-tolyl] tropane) is a tropane analog relatively selective for dopamine transporters in binding and uptake assays in vitro, with long-acting psychostimulant properties in vivo. To explore its utility in binding to dopamine
Publikováno v:
Molecular pharmacology. 57(5)
Previous studies had shown that the amplification factors for cannabinoid receptors, defined as the number of total G proteins activated per occupied receptor, differs between several rat brain regions. In this study, we sought to determine which spe
Publikováno v:
Neuropharmacology. 39(2)
Coupling of receptors to G-proteins can be assessed by the ability of specific agonists to stimulate [35S]GTPgammaS binding in both brain membranes and sections in the presence of excess GDP. In some brain regions, however, high basal activity makes
Publikováno v:
Synapse (New York, N.Y.). 35(4)
The sulfhydryl alkylating reagent N-ethylmaleimide (NEM) blocks opioid receptor binding and receptor/G-protein coupling. Sodium partially restores [(3)H]naloxone binding after inhibition by NEM to reveal sodium-dependent [(3)H]naloxone sites, defined
Autor:
S R, Letchworth, T, Sexton, S R, Childers, K E, Vrana, R A, Vaughan, H M, Davies, L J, Porrino
Publikováno v:
Journal of neurochemistry. 73(5)
This study describes a direct comparison of dopamine transporter (DAT) mRNA and protein, as well as its binding sites, in tissue from the same animals after chronic cocaine administration. Rats were treated twice daily with 25 mg/kg cocaine or with s