Search Results - "Rupniak, Nadia M J"

Affinity, potency, efficacy, and selectivity of neurokinin A analogs at human recombinant NK2 and NK1 receptors by Rupniak, Nadia M J, Perdona, Elisabetta, Griffante, Cristiana, Cavallini, Palmina, Sava, Anna, Ricca, Daniel J, Thor, Karl B, Burgard, Edward C, Corsi, Mauro

“…A series of peptide NK2 receptor agonists was evaluated for affinity, potency, efficacy, and selectivity at human recombinant NK2 and NK1 receptors expressed…”
Get full text

Effect of GR205171 on autonomic dysreflexia induced by colorectal distension in spinal cord injured rats by Rupniak, Nadia M. J., Fernandes, Silvia, Hou, Shaoping, Thor, Karl B., Marson, Lesley

“…Study design Preclinical pharmacology. Objectives To determine whether blocking substance P signaling attenuates the hypertension and bradycardia evoked by…”
Get full text

Colorectal and bladder prokinetic activity of [Lys 5 , MeLeu 9 , Nle 10 ]-NKA (4-10) after intranasal or sublingual delivery in dogs by Rupniak, Nadia M J, Katofiasc, Mary A, Bae, Jungeun, Thor, Karl B, Marson, Lesley

“…The feasibility of eliciting defecation and urination after intranasal (IN) or sublingual (SL) delivery of a small peptide NK2 receptor agonist, [Lys , MeLeu ,…”
Get more information

Prokinetic effects of the neurokinin NK2 receptor agonist [Lys5,MeLeu9,Nle10]-NKA(4–10) on bladder and colorectal activity in minipigs by Rupniak, Nadia M.J., Katofiasc, Mary A., Marson, Lesley, Ricca, Daniel J., Thor, Karl B., Burgard, Edward C.

“…The effects of the neurokinin NK2 receptor agonist [Lys5,MeLeu9,Nle10]-NKA(4–10) (LMN-NKA) on bladder and colorectal function were examined in minipigs. In…”
Get full text

Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives by Meurer, Laura C., Finke, Paul E., Owens, Karen A., Tsou, Nancy N., Ball, Richard G., Mills, Sander G., MacCoss, Malcolm, Sadowski, Sharon, Cascieri, Margaret A., Tsao, Kwei-Lan, Chicchi, Gary G., Egger, Linda A., Luell, Silvi, Metzger, Joseph M., MacIntyre, D. Euan, Rupniak, Nadia M.J., Williams, Angela R., Hargreaves, Richard J.

“…The optimization of a cyclopentane-based hNK1 antagonist scaffold will be discussed in the context of enhanced water-solubility, sub-nanomolar hNK1 binding…”
Get full text

NK1 receptor antagonists for depression: Why a validated concept was abandoned by Rupniak, Nadia M.J., Kramer, Mark S.

“…NK1 receptor antagonists were abandoned despite antidepressant efficacy in five randomized clinical trials. The loss of confidence may be attributed to the…”
Get full text

Prokinetic effects of neurokinin-2 receptor agonists on the bladder and rectum of rats with acute spinal cord transection by Marson, Lesley, Thor, Karl B., Katofiasc, Mary, Burgard, Edward C., Rupniak, Nadia M.J.

“…The suitability of various neurokinin-2 (NK2) receptor agonists and routes of administration to elicit on-demand voiding of the bladder and bowel, as future…”
Get full text

Substance P (Neurokinin 1) Receptor Antagonists Enhance Dorsal Raphe Neuronal Activity by Conley, Rachel K, Cumberbatch, Michael J, Mason, Glenn S, Williamson, David J, Harrison, Timothy, Locker, Karen, Swain, Christopher, Maubach, Karen, O'Donnell, Ruth, Rigby, Michael, Hewson, Louise, Smith, David, Rupniak, Nadia M. J

“…Substance P receptor [neurokinin 1 (NK1] antagonists (SPAs) represent a novel mechanistic approach to antidepressant therapy with comparable clinical efficacy…”
Get full text

Increased neurogenesis and brain-derived neurotrophic factor in neurokinin-1 receptor gene knockout mice by Morcuende, Sara, Gadd, Christopher A., Peters, Marco, Moss, Andrew, Harris, Elizabeth A., Sheasby, Anne, Fisher, Amy S., De Felipe, Carmen, Mantyh, Patrick W., Rupniak, Nadia M. J., Giese, K. Peter, Hunt, Stephen P.

“…It has previously been shown that chronic treatment with antidepressant drugs increases neurogenesis and levels of brain‐derived neurotrophic factor in the…”
Get full text

Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist by Hale, Jeffrey J, Mills, Sander G, MacCoss, Malcolm, Finke, Paul E, Cascieri, Margaret A, Sadowski, Sharon, Ber, Elzbieta, Chicchi, Gary G, Kurtz, Marc, Metzger, Joseph, Eiermann, George, Tsou, Nancy N, Tattersall, F. David, Rupniak, Nadia M. J, Williams, Angela R, Rycroft, Wayne, Hargreaves, Richard, MacIntyre, D. Euan

“…Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this…”
Get full text

Potency, efficacy, and selectivity of GR64349 at human recombinant neurokinin NK2 and NK1 receptors by Perdona, Elisabetta, Cavallini, Palmina, Sava, Anna, Griffante, Cristiana, Ricca, Daniel J., Thor, Karl B., Rupniak, Nadia M.J., Corsi, Mauro

“…•The affinity and potency of GR64349 for NK2 and NK1 receptors was examined.•Binding affinity was ˜1200-fold higher for NK2 than NK1 receptors.•Potency was…”
Get full text

Colorectal and cardiovascular effects of [Lys5,MeLeu9,Nle10]-NKA(4-10) in anesthetized macaques by Rupniak, Nadia M. J., Katofiasc, Mary, Burgard, Edward C., Thor, Karl B.

“…The effects of the tachykinin NK2 receptor agonist LMN-NKA ([Lys 5 ,MeLeu 9 ,Nle 10 ]-NKA (4-10) ) on colorectal and arterial blood pressure were examined in…”
Get full text

Chronic psychosocial stress in tree shrews : effect of the substance P (NK1 receptor) antagonist L-760735 and clomipramine on endocrine and behavioral parameters by VAN DER HART, Marieke G. C, DE BIURRUN, Gabriel, CZEH, Boldizsar, RUPNIAK, Nadia M. J, DEN BOER, Johan A, FUCHS, Eberhard

“…Substance P and its preferred receptor, the neurokinin 1 receptor (NK(1)R), have been proposed as possible targets for new antidepressant therapies, although…”
Get full text

NK2 and NK1 receptor-mediated effects of NKA and analogs on colon, bladder, and arterial pressure in anesthetized dogs by Rupniak, Nadia M. J., Katofiasc, Mary, Marson, Lesley, Thor, Karl B.

“…Tachykinin NK2 receptor (NK2R) agonists have potential to alleviate clinical conditions associated with bladder and gastrointestinal under activity. The…”
Get full text

The Hypothalamic–Pituitary–Adrenal Axis and Serotonin Metabolism in Individual Brain Nuclei of Mice with Genetic Disruption of the NK1 Receptor Exposed to Acute Stress by Culman, Juraj, Mühlenhoff, Stephan, Blume, Annegret, Hedderich, Jürgen, Lützen, Ulf, Hunt, Stephen P., Rupniak, Nadia M. J., Zhao, Yi

“…Mice lacking the substance P (SP) neurokinin-1 (NK1) receptor (NK1R−/−mice) were used to investigate whether SP affects serotonin (5-HT) function in the brain…”
Get full text

Distinct Mechanism for Antidepressant Activity by Blockade of Central Substance P Receptors by Kramer, Mark S., Cutler, Neal, Feighner, John, Shrivastava, Ram, Carman, John, Sramek, John J., Reines, Scott A., Liu, Guanghan, Snavely, Duane, Wyatt-Knowles, Edwina, Hale, Jeffrey J., Mills, Sander G., MacCoss, Malcolm, Swain, Christopher J., Harrison, Timothy, Hill, Raymond G., Hefti, Franz, Scolnick, Edward M., Cascieri, Margaret A., Chicchi, Gary G., Sadowski, Sharon, Williams, Angela R., Hewson, Louise, Smith, David, Carlson, Emma J., Hargreaves, Richard J., Nadia M. J. Rupniak

“…The localization of substance P in brain regions that coordinate stress responses and receive convergent monoaminergic innervation suggested that substance P…”
Get full text

The bradykinin B1 receptor antagonist B9858 inhibits a nociceptive spinal reflex in rabbits by Mason, Glenn S, Cumberbatch, Michael J, Hill, Raymond G, Rupniak, Nadia M J

“…There are two bradykinin receptor subtypes, designated B1 and B2. Whilst both have been implicated in nociception, it is believed that there is a low level of…”
Get more information

Species differences in tachykinin receptor distribution: Further evidence that the substance P (NK1) receptor predominates in human brain by Rigby, Michael, O'Donnell, Ruth, Rupniak, Nadia M.J.

“…Marked species differences in the distribution of central tachykinin receptors are reported but uncertainty remains about the ability of available ligands to…”
Get full text

5-Hydroxytryptamine (5-HT)1A Autoreceptor Adaptive Changes in Substance P (Neurokinin 1) Receptor Knock-Out Mice Mimic Antidepressant-Induced Desensitization by Froger, Nicolas, Gardier, Alain M, Moratalla, Rosario, Alberti, Israel, Lena, Isabelle, Boni, Claudette, De Felipe, Carmen, Rupniak, Nadia M. J, Hunt, Stephen P, Jacquot, Christian, Hamon, Michel, Lanfumey, Laurence

“…Antagonists at substance P receptors of the neurokinin 1 (NK1) type have been shown to represent a novel class of antidepressant drugs, with comparable…”
Get full text

New insights into the antidepressant actions of substance P (NK1 receptor) antagonists by Rupniak, Nadia M J

“…Considerable progress has been made in understanding the neural circuits involved the antidepressant and anxiolytic efficacy of substance P (NK, receptor)…”
Get more information