Furthermore, Salvinorin A acted as an uncompetitive inhibitor of DAMGO-stimulated guanosine 5'-O-(3-[(35)S]thio)-triphosphate binding. (erowid.org)
2007) Functional adenylyl cyclase inhibition in murine cardiomyocytes by 2 (3)-O- (N-methylanthraniloyl)-guanosine 5- (gamma-thio) triphosphate. (jenabioscience.com)
Heterotrimeric G(o)-proteins as well as guanosine 5'-3-O-(thio)triphosphate-liganded free alpha o-subunits are readily immunoprecipitated by these monoclonal antibodies. (researchgate.net)
They also enhanced binding of guanosine-5'-O-(3-thio)triphosphate and GTP azidoanilide to, and cholera toxin-catalyzed ADP-ribosylation of, Gi protein alpha subunits. (uni-regensburg.de)
Guanosine 5'-triphosphate (GTP) binding protein alpha subunits (Galpha(i)) are known to participate in the regulation of force in airway smooth muscle. (asahq.org)
One potential target is the function of systems regulated by guanosine 5′-triphosphate (GTP) binding proteins (G proteins). (asahq.org)
3. Changes in the cannabinoid receptor binding, G protein coupling, and cyclic AMP cascade in the CNS of rats tolerant to and dependent on the synthetic cannabinoid compound CP55,940. (nih.gov)
5. In vivo characterization of the specific cannabinoid receptor antagonist, SR141716A: behavioral and cellular responses after acute and chronic treatments. (nih.gov)
Receptor6
In the United States, CB1 receptor agonists of the 3-(1-naphthoyl)pyrrole class such as JWH-030 are Schedule I Controlled Substances. (wikipedia.org)
Total adenosine A(1) receptor number, determined by radioligand binding assay, using [(3)H]DPCPX, was significantly increased in AD cases in early and advanced stages without differences with the progression of the disease. (nih.gov)
Salvinorin A [(2S,4aR,6aR,7R,9S,10aS,10bR)-9-(acetyloxy)-2-(3-furanyl)-dodecahydro-6a,10b-dimethyl-4,10-dioxo-2h-naphtho[2,1-c]pyran-7-carboxylic acid methyl ester] is a hallucinogenic kappa-opioid receptor agonist that lacks the usual basic nitrogen atom present in other known opioid ligands. (erowid.org)
Saturation binding studies with [(3)H]DAMGO showed that Salvinorin A (10 and 30 muM) decreased the mu-receptor B(max) and increased the K(d) in a dose-dependent nonlinear manner. (erowid.org)
8. Loss of cannabinoid-stimulated guanosine 5'-O-(3-[(35)S]Thiotriphosphate) binding without receptor down-regulation in brain regions of anandamide-tolerant rats. (nih.gov)
We compared the effects of 2-(3-chlorophenyl)-histamine (CPH) [2-[2-(3-chlorophenyl)-1H-imidazol-4-yl] ethanamine], one of the most potent and selective H1 receptor agonists presently available, with those of histamine and N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP) in these cells. (uni-regensburg.de)
The possible involvement of guanine nucleotide binding proteins in dihydropyridine binding has been investigated by studying the effects of guanosine 5'-0-(3-thiotriphosphate) (GTPγS) and guanosine 5,-0-(2-thiodiphosphate)(GDPβS) on binding parameters. (edu.au)
Antagonist1
R was detected with the antagonist 125 I-astressin with 30 μM guanosine 5′- O -(3-thiotriphosphate present, and RG detected using 125 I-sauvagine. (aspetjournals.org)
In addition, increased numbers of adenosine A(2A) receptors were observed in AD samples as determined by a binding assay using [(3)H]ZM 241385 as a radioligand and by Western blot. (nih.gov)
Inhibition1
32P]Pi release from exogenous [5-32P]Ins(1,4,5)P3 was also inhibited by DL-InsP3S3, DL-InsP3S and DL-InsP3, with half-maximal inhibition at approximately 50 microM, 160 microM and 240 microM respectively. (ox.ac.uk)
Membranes1
Consistent data were obtained from GPR82-mediated binding analysis of guanosine-5'-O-(3-thiotriphosphate) to cell membranes. (bvsalud.org)
Acid1
Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. (nih.gov)
Partially inhibited2
Salvinorin A partially inhibited [(3)H]Tyr-d-Ala-Gly-N-Me-Phe-Gly-ol (DAMGO) (0.5, 2.0, and 8.0 nM) binding with E(MAX) values of 78.6, 72.1, and 45.7%, respectively, and EC(50) values of 955, 1124, and 4527 nM, respectively. (erowid.org)
Reciprocal effects at the R state were demonstrated using [ 3 H]NBI 35965: agonist peptides only partially inhibited binding (by 13-40%) and accelerated [ 3 H]NBI 35965 dissociation. (aspetjournals.org)
Effects3
12. Differential effects of haloperidol and clozapine on [(3)H]cAMP binding, protein kinase A (PKA) activity, and mRNA and protein expression of selective regulatory and catalytic subunit isoforms of PKA in rat brain. (nih.gov)
These actions were approximately ten times more potent than the effects of these compounds on [3H]inositol phosphate accumulation, indicating that homogenous mixing of exogenous and cell-membrane-derived Ins(1,4,5)P3 does not occur. (ox.ac.uk)
In contrast, the effects of synthetic DL-InsP3 and D-Ins(1,4,5)P3 are due to isotopic dilution. (ox.ac.uk)
Potent3
2003) 2' (3')-O- (N-methylanthraniloyl)-substituted GTP analogs: a novel class of potent competitive adenylyl cyclase inhibitors. (jenabioscience.com)
Whilst DL-InsP3S3 was the most potent inhibitor of dephosphorylation of exogenous or cell-membrane-derived Ins(1,4,5)P3, it was the weakest inhibitor of 3-kinase-catalysed Ins(1,4,5)P3 phosphorylation. (ox.ac.uk)
Similarly, although approximately 50 times less potent than DL-InsP3S3, 2,3-diphosphoglycerate inhibited Ins(1,4,5)P3 5-phosphatase activity and was apparently without effect of Ins(1,4,5)P3 3-kinase activity. (ox.ac.uk)
Dissociation2
Kinetic experiments demonstrated that Salvinorin A altered the dissociation kinetics of both [(3)H]DAMGO and [(3)H]diprenorphine binding to mu receptors. (erowid.org)
Binding was also saturable and of high affinity with dissociation constants (Kd) in the low picomolar range and was significantly inhibited in the presence of 10(-4)M guanosine 5'-0-(3-thiotriphosphate) (GTP gamma S) and 150 mM NaCl in all regions examined, indicating the presence of high affinity G-protein coupled melatonin receptors. (elsevierpure.com)
Activity4
2011) Structure-activity relationships for the interactions of 2'- and 3'- (O)- (N-methyl)anthraniloyl-substituted purine and pyrimidine nucleotides with mammalian adenylyl cyclases. (jenabioscience.com)
In addition, edelfosine (1-O-octadecyl-2-O-methyl-sn-glycero-3-phosphocholine), an artificial lysophospholipid with a cationic head group that exerts antitumor activity, inhibited the Gi protein activation by GPR82. (bvsalud.org)
Two endogenous lysophospholipids with cationic head groups, lysophosphatidylcholine (1-oleoyl-sn-glycero-3-phosphocholine) and lysophosphatidylethanolamine (1-oleoyl-sn-glycero-3-phosphoethanolamine), also exhibited GPR82 inhibitory activity, albeit weaker than edelfosine. (bvsalud.org)
The PLD activity of streptolysin O-permeabilized, cytosol- depleted rabbit neutrophils was significantly enhanced when the permeabilized cells were reconstituted with bovine braincytosol in the presence of guanosine 5'-O-(3-thiotriphosphate) (GTPγS), whereas there was little activation of the enzyme in the absence of cytosol. (elsevierpure.com)
Cells2
Multiple sections from 3 to 5 mice per group, separated by at least 200 μm from each section, were assessed for signal intensity and the number of nuclear p27- or proliferating cell nuclear antigen (PCNA)-positive (PCNA + ) β-cells with LSM Image Browser software (Carl Zeiss). (medscape.com)
The cross-sectional areas of pancreata and β-cells were determined from multiple sections ( n = 5 mice per group), separated by at least 200 μm from each section, using LSM Image Browser software. (medscape.com)
Findings2
Similar findings were observed in rat brain with [(3)H]DAMGO. (erowid.org)
These findings indicate that DL-InsP3S3 and DL-InsP3S inhibit Ins(1,4,5)P3 5-phosphatase. (ox.ac.uk)
Journal2
Pflugers Archiv European Journal of Physiology , 436 (3), 494-496. (ewha.ac.kr)
The zebrafish embryo is an ideal model system for studying PGC migration due to 1) the transparency of the embryo, allowing in vivo analyses of cell migration and development, 2) the availability of various mutant stocks and the morpholino antisense oligo nucleotide gene knockdown system, and 3) the availability of PGC marker genes, for which localisation and functions are well characterised. (exeter.ac.uk)
Publication1
MolPharm articles become freely available 12 months after publication, and remain freely available for 5 years. (aspetjournals.org)
Study1
[ 16 ] The study used male 2- to 3-month-old CB1R +/+ and CB1R −/− mice. (medscape.com)
Cases1
[ 17 ] After antigen unmasking, the slides were incubated with primary antibodies (Supplementary Table 1), followed by secondary antibodies (Invitrogen, Carlsbad, CA) along with TO-PRO-3 (Invitrogen), in some cases, for nuclear staining. (medscape.com)