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Your search keyword '"April Smith Torhan"' showing total 5 results
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5 results on '"April Smith Torhan"'

1. Identification of 3-substituted N-benzhydryl-nortropane analogs as nociceptin receptor ligands for the management of cough and anxiety

Author

Geoffrey B. Varty, Shu-Wei Yang, Zheng Tan, Ahmad Fawzi, Sherry Lu, John C. Anthes, William J. Greenlee, Ginny D. Ho, Deen Tulshian, April Smith-Torhan, Hongtao Zhang, John A. Hey, Xiomara Fernandez, and Robbie L. McLeod

Subjects
Nortropanes, Stereochemistry, medicine.drug_class, Chemistry, Pharmaceutical, Guinea Pigs, Clinical Biochemistry, NOP, Administration, Oral, Pharmaceutical Science, Carboxamide, Peptide, Anxiety, Ligands, Biochemistry, Chemical synthesis, Anxiolytic, Nociceptin Receptor, Structure-Activity Relationship, Drug Discovery, medicine, Animals, Molecular Biology, chemistry.chemical_classification, Molecular Structure, Chemistry, Ligand, Organic Chemistry, Antitussive Agents, Kinetics, Nociceptin receptor, Anti-Anxiety Agents, Cough, Antitussive Agent, Drug Design, Receptors, Opioid, Molecular Medicine
Abstract

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.

Published
2009
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2. Cloning and characterization of the hamster and guinea pig nicotinic acid receptors

Author

April Smith Torhan, Boonlert Cheewatrakoolpong, Lia Kwee, and Scott Greenfeder

Subjects
Guinea Pigs, Molecular Sequence Data, Hamster, CHO Cells, niacin, QD415-436, Receptors, Nicotinic, Biology, Biochemistry, Guinea pig, Cricetulus, Endocrinology, Cricetinae, Animals, Humans, Amino Acid Sequence, Cloning, Molecular, Receptor, Peptide sequence, chemistry.chemical_classification, Chinese hamster ovary cell, Cell Biology, GPR109A, Molecular biology, Amino acid, Dissociation constant, Nicotinic agonist, chemistry, Sequence Alignment, HM74A
Abstract

In this study, we present the identification and characterization of hamster and guinea pig nicotinic acid receptors. The hamster receptor shares approximately 80-90% identity with the nucleotide and amino acid sequences of human, mouse, and rat receptors. The guinea pig receptor shares 76-80% identity with the nucleotide and amino acid sequences of these other species. [(3)H]nicotinic acid binding affinity at guinea pig and hamster receptors is similar to that in human (dissociation constant = 121 nM for guinea pig, 72 nM for hamster, and 74 nM for human), as are potencies of nicotinic acid analogs in competition binding studies. Inhibition of forskolin-stimulated cAMP production by nicotinic acid and related analogs is also similar to the activity in the human receptor. Analysis of mRNA tissue distribution for the hamster and guinea pig nicotinic acid receptors shows expression across a number of tissues, with higher expression in adipose, lung, skeletal muscle, spleen, testis, and ovary.

Published
2007
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3. Synthesis and structure–activity relationships of 4-hydroxy-4-phenylpiperidines as nociceptin receptor ligands: Part 1

Author

Ginny D. Ho, Deen Tulshian, Ahmad Fawzi, William J. Greenlee, Hongtao Zhang, April Smith Torhan, and Ana Bercovici

Subjects
Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Neuropeptide, Peptide, CHO Cells, Ligands, Biochemistry, Chemical synthesis, Nociceptin Receptor, Structure-Activity Relationship, Cricetulus, Piperidines, Cricetinae, Drug Discovery, Animals, Humans, Molecular Biology, G protein-coupled receptor, chemistry.chemical_classification, Molecular Structure, Chemistry, Ligand, Organic Chemistry, In vitro, Nociceptin receptor, Receptors, Opioid, Molecular Medicine
Abstract

A series of 4-hydroxy-4-phenylpiperidines have been synthesized and bind to the nociceptin receptor with high affinity. The synthesis and structure-activity relationships at the N-1 and C-4 are described.

Published
2007
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4. Hydrazides of clozapine: A new class of D1 dopamine receptor subtype selective antagonists

Author

Thavalakulamgara K. Sasikumar, Duane A. Burnett, Jean E. Lachowicz, Ahmad Fawzi, Hongtao Zhang, and April Smith-Torhan

Subjects
Clinical Biochemistry, Pharmaceutical Science, Pharmacology, Biochemistry, Chemical synthesis, Structure-Activity Relationship, Dopamine, Dopamine receptor D2, Drug Discovery, medicine, Clozapine, Molecular Biology, Molecular Structure, Receptors, Dopamine D2, Chemistry, Receptors, Dopamine D1, Organic Chemistry, Antagonist, In vitro, Dopamine D2 Receptor Antagonists, Hydrazines, Dopamine receptor, Dopamine Antagonists, Molecular Medicine, Selectivity, medicine.drug
Abstract

Acylated and aroylated hydrazinoclozapines are highly potent dopamine D1 antagonists that show remarkable selectivity over other dopamine receptors. The most potent compound in this series is the 2,6-dimethoxybenzhydrazide 33 with a D1 Ki of 1.6 nM and 212-fold selectivity over D2 receptor.

Published
2006
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5. Nociceptin inhibits capsaicin-induced bronchoconstriction in isolated guinea pig lung

Author

Julius J. Matasi, Robert W. Egan, Maria A. Rivelli, John A. Hey, April Smith-Torhan, Deen Tulshian, Lawrence Benbow, Hongtao Zhang, Ahmad Fawzi, and Michel R. Corboz

Subjects
Agonist, medicine.medical_specialty, medicine.drug_class, Bronchoconstriction, Narcotic Antagonists, Guinea Pigs, CHO Cells, (+)-Naloxone, In Vitro Techniques, Sulfur Radioisotopes, Nociceptin Receptor, Piperidines, Opioid receptor, Cricetinae, Internal medicine, medicine, Animals, Opioid peptide, Lung, Pharmacology, Orphan receptor, Naloxone, Chemistry, Nociceptin receptor, Endocrinology, Opioid Peptides, Opioid, Guanosine 5'-O-(3-Thiotriphosphate), Receptors, Opioid, Benzimidazoles, Capsaicin, medicine.symptom, medicine.drug
Abstract

The isolated perfused guinea pig lung was used to investigate the effect of nociceptin against bronchoconstriction elicited by endogenous and exogenous tachykinins. The opioid receptor-like 1 (ORL1) receptor agonist, nociceptin/orphanin FQ (0.001-1 microM) produced a dose-related inhibition of the capsaicin-induced bronchoconstriction (10(-5)-10(3) microg) in isolated guinea pig lung (P

Published
2000
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