Search Results - "Armstrong, Scott R"
-
1
Concomitant Angiotensin AT1 Receptor Antagonism and Neprilysin Inhibition Produces Omapatrilat-like Antihypertensive Effects Without Promoting Tracheal Plasma Extravasation in the Rat
Published in Journal of cardiovascular pharmacology (01-04-2011)“…Dual inhibition of angiotensin-converting enzyme (ACE) and neprilysin (NEP) by drugs such as omapatrilat produces superior antihypertensive efficacy but cause…”
Get full text
Journal Article -
2
Discovery of Axelopran (TD-1211): A Peripherally Restricted μ‑Opioid Receptor Antagonist
Published in ACS medicinal chemistry letters (12-12-2019)“…The effects of opioids in the central nervous system (CNS) provide significant benefit in the treatment of pain but can also lead to physical dependence and…”
Get full text
Journal Article -
3
Discovery of TD-8954, a clinical stage 5-HT4 receptor agonist with gastrointestinal prokinetic properties
Published in Bioorganic & medicinal chemistry letters (15-07-2013)“…The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the…”
Get full text
Journal Article -
4
The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-06-2013)“…The clinical efficacy of opioid receptor antagonists for the treatment of opioid-induced constipation (OIC) is established. Peripherally selective antagonists…”
Get full text
Journal Article -
5
The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-06-2013)“…The in vivo preclinical pharmacodynamic profile of TD-1211, a selective opioid receptor antagonist currently under development for the treatment of…”
Get full text
Journal Article -
6
Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…Utilization of Theravance’s multivalent approach to drug discovery towards 5-HT4 receptor agonists with a focus on identification of neutral (non-charged at…”
Get full text
Journal Article -
7
The Pharmacology of TD-8954, a Potent and Selective 5-HT4 Receptor Agonist with Gastrointestinal Prokinetic Properties
Published in Frontiers in pharmacology (01-01-2011)“…This study evaluated the in vitro and in vivo pharmacological properties of TD-8954, a potent and selective 5-HT 4 receptor agonist. TD-8954 had high affinity…”
Get full text
Journal Article -
8
Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: Clinical compound TD-2749
Published in Bioorganic & medicinal chemistry letters (15-07-2012)“…Further application of our multivalent approach to drug discovery directed to 5-HT4 receptor agonists is described. Optimization of the linker and secondary…”
Get full text
Journal Article -
9
A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT4 Receptor Agonists
Published in Journal of medicinal chemistry (10-09-2009)“…5-HT4 receptor agonists such as tegaserod have demonstrated efficacy in the treatment of constipation predominant irritable bowel syndrome (IBS-C), a highly…”
Get full text
Journal Article -
10
Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist
Published in European journal of pharmacology (01-03-2009)“…Existing antimuscarinic drugs for overactive bladder have high affinity for M 3/M 1 muscarinic receptors and consequently produce M 3/M 1-mediated adverse…”
Get full text
Journal Article -
11
-
12
Measurement of 5-HT4 receptor-mediated esophageal responses by digital sonomicrometry in the anesthetized rat
Published in Journal of pharmacological and toxicological methods (01-05-2006)“…In vitro studies have demonstrated a 5-HT4 receptor-mediated relaxation of the pre-contracted rat esophagus. However, it is unclear whether 5-HT4 receptor…”
Get full text
Journal Article -
13
Pharmacological analysis of the interaction of antimuscarinic drugs at M2 and M3 muscarinic receptors in vivo using the pithed rat assay
Published in Naunyn-Schmiedeberg's archives of pharmacology (2008)“…Muscarinic receptor antagonists form the mainstay of the therapeutic options for airway, bladder, and gastrointestinal smooth muscle disorders. Both M 2 and M…”
Get full text
Journal Article -
14
-
15
Pharmacological analysis of the interaction of antimuscarinic drugs at M(2) and M(3) muscarinic receptors in vivo using the pithed rat assay
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-01-2008)“…Muscarinic receptor antagonists form the mainstay of the therapeutic options for airway, bladder, and gastrointestinal smooth muscle disorders. Both M(2) and…”
Get full text
Journal Article -
16
A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT 4 Receptor Agonists
Published in Journal of medicinal chemistry (10-09-2009)Get full text
Journal Article -
17
Discovery of TD-8954, a clinical stage 5-HT(4) receptor agonist with gastrointestinal prokinetic properties
Published in Bioorganic & medicinal chemistry letters (15-07-2013)“…The discovery of a series of 5-HT4 receptor agonists based on a novel 2-alkylbenzimidazole aromatic core is described. Optimization of the 2-substituent of the…”
Get full text
Journal Article -
18
Measurement of 5-HT sub(4) receptor-mediated esophageal responses by digital sonomicrometry in the anesthetized rat
Published in Journal of pharmacological and toxicological methods (01-06-2006)“…Introduction In vitro studies have demonstrated a 5-HT sub(4) receptor- mediated relaxation of the pre-contracted rat esophagus. However, it is unclear whether…”
Get full text
Journal Article -
19
Measurement of 5-HT 4 receptor-mediated esophageal responses by digital sonomicrometry in the anesthetized rat
Published in Journal of pharmacological and toxicological methods (2006)“…In vitro studies have demonstrated a 5-HT 4 receptor-mediated relaxation of the pre-contracted rat esophagus. However, it is unclear whether 5-HT 4 receptor…”
Get full text
Journal Article -
20
Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…Utilization of Theravance's multivalent approach to drug discovery towards 5-HT(4) receptor agonists with a focus on identification of neutral (non-charged at…”
Get full text
Journal Article