codeine has been researched along with Cough* in 4 studies
4 other study(ies) available for codeine and Cough
| Article | Year |
|---|---|
Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety.
A series of nortropane analogs based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. The synthesis and structure-activity relationships around the C-3 nortropane substitution are described. From the SAR study and hPXR screening effort, compound 15 was identified to possess potent oral antitussive and anxiolytic-like activities in the guinea pig models. Topics: Administration, Oral; Animals; Anti-Anxiety Agents; Antitussive Agents; Anxiety; Chemistry, Pharmaceutical; Cough; Drug Design; Guinea Pigs; Kinetics; Ligands; Molecular Structure; Nociceptin Receptor; Nortropanes; Receptors, Opioid; Structure-Activity Relationship | 2009 |
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
The discovery of 1 as a high-affinity ligand for the nociceptin receptor has led to the synthesis of a series of tropane (8-methyl-8-azabicyclo[3.2.1]octane) derivatives as optimized ligands. These compounds exhibit high affinity for the nociceptin receptor, moderate to excellent selectivity over the opioid mu receptor, and behave as full agonists. In this Letter, we present the synthesis and highlight the structure-activity relationship of tropane derivatives culminating in the identification of 24 and 32 as potent and orally active antitussive and anxiolytic agents. The in vitro and in vivo activities, pharmacokinetic profile, and the hPXR activity, which predicts the potential 3A4 induction in human, are disclosed. Topics: Animals; Anti-Anxiety Agents; Antitussive Agents; Anxiety; Capsaicin; Chemistry, Pharmaceutical; Cough; Drug Design; Guinea Pigs; Humans; Ligands; Nociceptin Receptor; Pregnane X Receptor; Receptors, Opioid; Receptors, Steroid; Structure-Activity Relationship; Tropanes | 2009 |
Discovery of orally active 3-pyridinyl-tropane as a potent nociceptin receptor agonist for the management of cough.
A series of 3-pyridinyl-tropane analogues based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high affinity. From the SAR study and our lead optimization efforts, compound 10 was found to possess potent oral antitussive activity in the capsaicin-induced guinea pig model. The rationale for compound selection and the biological profile of the optimized lead (10) are disclosed. Topics: Administration, Oral; Animals; Antitussive Agents; Cough; Dogs; Drug Discovery; Guinea Pigs; Humans; Nociceptin Receptor; Pregnane X Receptor; Pyridines; Rats; Receptors, Opioid; Receptors, Steroid; Structure-Activity Relationship; Trans-Activators; Transcriptional Regulator ERG; Tropanes; Vocalization, Animal | 2009 |
Synthesis and antitussive activity of aminotetra- (and -hexa-) hydrodibenzofurans.
The synthesis of a novel series of antitussive agents is described. Two series of amino-substituted tetra- and hexahydrodibenzofurans were prepared and examined for antitussive activity in the guinea pig after cough elicited by electrical stimulation of the vagus nerve. A significant level of activity, comparable with that of codeine, was found in the 4alpha-amino series. The 4-methylpiperazin-1-ylpropionamide (28) was found to be the most active of the compounds synthesized and was equipment with codeine. The effects of structural modification upon antitussive activity were investigated in numerous analogues but no enhancement of activity was achieved over that of 28. Topics: Animals; Antitussive Agents; Benzofurans; Cough; Electric Stimulation; Guinea Pigs; Male; Structure-Activity Relationship; Vagus Nerve | 1977 |