Search Results - "YAMAMURA, H. I"

Extremely long-lasting antagonistic actions of nor-binaltorphimine (nor-BNI) in the mouse tail-flick test by Horan, P, Taylor, J, Yamamura, H I, Porreca, F

“…The duration of antagonistic action of nor-binaltorphimine (nor-BNI), a kappa antagonist, of antinociception resulting from selective opioid agonists, was…”
Get more information

Plasmon resonance studies of agonist/antagonist binding to the human delta-opioid receptor: new structural insights into receptor-ligand interactions by Salamon, Z, Cowell, S, Varga, E, Yamamura, H I, Hruby, V J, Tollin, G

“…Structural changes accompanying the binding of ligands to the cloned human delta-opioid receptor immobilized in a solid-supported lipid bilayer have been…”
Get full text

Enkephalin Glycopeptide Analogues Produce Analgesia with Reduced Dependence Liability by Bilsky, Edward J, Egleton, Richard D, Mitchell, Scott A, Palian, Michael M, Davis, Peg, Huber, Jason D, Jones, Heather, Yamamura, Henry I, Janders, Jacqueline, Davis, Thomas P, Porreca, Frank, Hruby, Victor J, Polt, Robin

“…Endogenous peptides (e.g. enkephalins) control many aspects of brain function, cognition, and perception. The use of these neuroactive peptides in diverse…”
Get full text

Cannabinoid CB1 receptor expression, activation and detection of endogenous ligand in trabecular meshwork and ciliary process tissues by STAMER, W. D, GOLIGHTLY, S. F, HOSOHATA, Y, RYAN, E. P, PORTER, A. C, VARGA, E, NOECKER, R. J, FELDER, C. C, YAMAMURA, H. I

Get full text

Molecular biology and pharmacology of cloned opioid receptors by Knapp, R J, Malatynska, E, Collins, N, Fang, L, Wang, J Y, Hruby, V J, Roeske, W R, Yamamura, H I

“…The cloning and expression of DNA for the three major opioid receptor types (mu, delta, and kappa) present new research opportunities for the characterization…”
Get more information

Antinociceptive profile of biphalin, a dimeric enkephalin analog by Horan, P J, Mattia, A, Bilsky, E J, Weber, S, Davis, T P, Yamamura, H I, Malatynska, E, Appleyard, S M, Slaninova, J, Misicka, A

“…The dimeric enkephalin biphalin (Try-D-Ala-Gly-Phe-NH)2 was evaluated in mice using antinociceptive, gastrointestinal and physical dependence paradigms and…”
Get more information

Glycopeptide Enkephalin Analogues Produce Analgesia in Mice: Evidence for Penetration of the Blood-Brain Barrier by Polt, Robin, Porreca, Frank, Szabo, Lajos Z., Bilsky, Edward J., Davis, Peg, Abbruscato, Thomas J., Davis, Thomas P., Horvath, Robert, Yamamura, Henry I., Hruby, Victor J.

“…Most peptides have not proved useful as neuroactive drugs because they are blocked by the blood-brain barrier and do not reach their receptors within the…”
Get full text

New endomorphin analogs with mu-agonist and delta-antagonist properties by Tóth, G., Keresztes, A., Tömböly, Cs, Péter, A., Fülöp, F., Tourwé, D., Navratilova, E., Varga, É., Roeske, W. R., Yamamura, H. I., Szucs, M., Borsodi, A.

“…Endomorphins (endomorphin-1,H-Tyr-Pro-Trp-Phe-NH 2 ,endomorphin-2, Tyr-Pro-Phe-Phe-NH ) are potent and selective µ-opioid receptor agonists. In order to…”
Get full text

Whole body and brain distribution of [3H]cyclic [D-Pen2,D-Pen5] enkephalin after intraperitoneal, intravenous, oral and subcutaneous administration by Weber, S J, Greene, D L, Hruby, V J, Yamamura, H I, Porreca, F, Davis, T P

“…The route of administration of a given drug can have a significant influence upon whole body distribution. The present study examined whole body distribution…”
Get more information

Relative efficacies of cannabinoid CB1 receptor agonists in the mouse brain by BURKEY, T. H, QUOCK, R. M, CONSROE, P, EHLERT, F. J, HOSOHATA, Y, ROESKE, W. R, YAMAMURA, H. I

“…We measured (-)-5-(1,1-dimethylheptyl)-2-[5-hydroxy-2-(3-hydroxypropyl)cyclohe xyl]-phenol (CP 55,940)-, (-)11-OH-delta8-tetrahydrocannabinol-dimethylheptyl…”
Get full text

Characterization of [3H]naltrindole binding to delta opioid receptors in mouse brain and mouse vas deferens: evidence for delta opioid receptor heterogeneity by Fang, L, Knapp, R J, Horvath, R, Matsunaga, T O, Haaseth, R C, Hruby, V J, Porreca, F, Yamamura, H I

“…Naltrindole (NTI) is a potent and selective nonpeptide delta opioid receptor antagonist. This study reports on the binding characteristics of [3H]NTI (specific…”
Get more information

De Novo Design, Synthesis, and Biological Activities of High-Affinity and Selective Non-Peptide Agonists of the δ-Opioid Receptor by Liao, Subo, Alfaro-Lopez, Josue, Shenderovich, Mark D, Hosohata, Keiko, Lin, Jun, Li, Xiaoping, Stropova, Dagmar, Davis, Peg, Jernigan, Kevin A, Porreca, Frank, Yamamura, Henry I, Hruby, Victor J

“…On the basis of the structure−activity relationships of δ-opioid-selective peptide ligands and on a model of the proposed bioactive conformation for a potent…”
Get full text

Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin by Lipkowski, Andrzej W., Misicka, Aleksandra, Davis, Peg, Stropova, Dagmar, Janders, Jacqueline, Lachwa, Magdalena, Porreca, Frank, Yamamura, Henry I., Hruby, Victor J.

“…The synthesis and biological activity of two fragments of the very potent opioid peptide biphalin, showed that Tyr-D-Ala-Gly-Phe-NH-NH<-Phe is the minimal…”
Get full text

Endomorphin-1 and endomorphin-2 are partial agonists at the human μ-opioid receptor by Hosohata, Keiko, Burkey, Thomas H, Alfaro-Lopez, Josue, Varga, Eva, Hruby, Victor J, Roeske, William R, Yamamura, Henry I

“…Recently two tetrapeptide ligands that bind preferentially to the μ-opioid receptor were identified and named endomorphin-1 and endomorphin-2. We examined the…”
Get full text

Distribution and analgesia of [3H][D-Pen2, D-Pen5]enkephalin and two halogenated analogs after intravenous administration by Weber, S J, Greene, D L, Sharma, S D, Yamamura, H I, Kramer, T H, Burks, T F, Hruby, V J, Hersh, L B, Davis, T P

“…To improve pharmacological characteristics of the delta-selective, cyclic peptide [D-Pen2, D-Pen5]enkephalin (DPDPE), modification by halogenation at the Phe4…”
Get more information

AM630 antagonism of cannabinoid-stimulated [ 35S]GTPγS binding in the mouse brain by Hosohata, Yoshiaki, Quock, Raymond M., Hosohata, Keiko, Makriyannis, Alexandros, Consroe, Paul, Roeske, William R., Yamamura, Henry I.

“…This research was designed to determine the action of the novel aminoalkylindole AM630 (6-iodo-pravadoline) at the cannabinoid receptor by studying its…”
Get full text

Assessment of Stereoselectivity of Trimethylphenylalanine Analogues of δ‐Opioid [D‐Pen2,D‐Pen5]‐Enkephalin by Witt, Ken A., Slate, Cheryl A., Egleton, Richard D., Huber, Jason D., Yamamura, Henry I., Hruby, Victor J., Davis, Thomas P.

“…: [D‐Pen2,D‐Pen5]‐Enkephalin (DPDPE) is an enzymatically stable δ‐opioid receptor‐selective peptide, which was modified by the trimethylation of the Phe4…”
Get full text

Exploring the Structure−Activity Relationships of [1-(4-tert-Butyl-3‘-hydroxy)benzhydryl-4-benzylpiperazine] (SL-3111), A High-Affinity and Selective δ-Opioid Receptor Nonpeptide Agonist Ligand by Alfaro-Lopez, Josue, Okayama, Toru, Hosohata, Keiko, Davis, Peg, Porreca, Frank, Yamamura, Henry I, Hruby, Victor J

“…SL-3111 [1-(4-tert-butyl-3‘-hydroxy)benzhydryl-4-benzylpiperazine] is a de novo designed, high-affinity and selective nonpeptide peptidomimetic agonist of the…”
Get full text

Opiate Aromatic Pharmacophore Structure−Activity Relationships in CTAP Analogues Determined by Topographical Bias, Two-Dimensional NMR, and Biological Activity Assays by Bonner, G. Gregg, Davis, Peg, Stropova, Dagmar, Edsall, Sidney, Yamamura, Henry I, Porreca, Frank, Hruby, Victor J

“…Topographically constrained analogues of the highly μ-opioid-receptor-selective antagonist CTAP (H-d-Phe-c[Cys-Tyr-d-Trp-Arg-Thr-Pen]-Thr-NH2, 1) were prepared…”
Get full text

Enhancement of morphine antinociception by a CCKB antagonist in mice is mediated via opioid delta receptors by Vanderah, T W, Bernstein, R N, Yamamura, H I, Hruby, V J, Porreca, F

“…This study investigated the possible involvement of opioid delta receptors in the modulation of morphine antinociceptive potency produced by L365,260 a CCKB…”
Get more information