J. Hadcock

发表

Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.

A. Kalgutkar, J. Warmus, D. Hepworth, 2013, ACS medicinal chemistry letters.

Identification of a critical aspartate residue in transmembrane domain three necessary for the binding of somatostatin to the somatostatin receptor SSTR2.

J. Strnad, J. Hadcock, 1995, Biochemical and biophysical research communications.

Supraphysiologic Administration of GDF11 Induces Cachexia in Part by Upregulating GDF15.

D. Glass, Juli E Jones, Chenguang Gong, 2018, Cell reports.

Agonist Regulation of Gene Expression of Adrenergic Receptors and G Proteins

C. Malbon, J. Hadcock, 1993, Journal of neurochemistry.

Regulation of receptor expression by agonists: transcriptional and post-transcriptional controls

J. Hadcock, Craig C. Maibon, 1991, Trends in Neurosciences.

AdipoR1 and 2 are expressed on warm sensitive neurons of the hypothalamic preoptic area and contribute to central hyperthermic effects of adiponectin

T. Bártfai, M. Marcondes, B. Conti, 2011, Brain Research.

Downregulation of GPR83 in the hypothalamic preoptic area reduces core body temperature and elevates circulating levels of adiponectin.

T. Bártfai, B. Conti, G. Moroncini, 2012, Metabolism: clinical and experimental.

A Selective Cannabinoid-1 Receptor Antagonist, PF-95453, Reduces Body Weight and Body Fat to a Greater Extent than Pair-Fed Controls in Obese Monkeys

B. Auerbach, K. Kavanagh, H. J. Harwood, 2010, Journal of Pharmacology and Experimental Therapeutics.

Somatostatin acts by inhibiting the cyclic 3',5'-adenosine monophosphate (cAMP)/protein kinase A pathway, cAMP response element-binding protein (CREB) phosphorylation, and CREB transcription potency.

J. Tentler, A. Gutierrez-Hartmann, J. Hadcock, 1997, Molecular endocrinology.

In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB(1) receptor antagonist for the management of obesity.

D. Scott, D. Hargrove, R. L. Dow, 2010, Biochemical and biophysical research communications.

New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.

D. Scott, P. Iredale, S. Sakya, 2006, Bioorganic & medicinal chemistry letters.

Pharmacological characterization of the rat A2a adenosine receptor functionally coupled to the yeast pheromone response pathway.

M. Pausch, J. Strnad, J. Hadcock, 1996, Molecular pharmacology.

Supraphysiologic Administration of GDF11 Induces Cachexia in Part by Upregulating GDF15.

D. Glass, Juli E Jones, Chenguang Gong, 2018, Cell reports.

Ccl22/MDC, is a prostaglandin dependent pyrogen, acting in the anterior hypothalamus to induce hyperthermia via activation of brown adipose tissue.

T. Bártfai, B. Morrison, M. Sánchez-Alavez, 2011, Cytokine.

The CNS-penetrant soluble guanylate cyclase stimulator CYR119 attenuates markers of inflammation in the central nervous system

M. Currie, C. Winrow, Juli E Jones, 2021, Journal of Neuroinflammation.

Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin.

S. Toler, B. Lefker, J. A. Ragan, 2003, Bioorganic & medicinal chemistry.

Identification and characterization of novel somatostatin antagonists.

M. Pausch, J. Strnad, J. Hadcock, 1996, Molecular pharmacology.

Quantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) Receptor Antagonist

D. Scott, P. Iredale, Xingrong Liu, 2010, BMC pharmacology.

Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.

D. Scott, P. Iredale, C. Nduaka, 2009, Journal of medicinal chemistry.

Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.

T. Maurer, D. Hargrove, R. L. Dow, 2004, Bioorganic & medicinal chemistry letters.

Rat somatostatin receptor type 1 couples to G proteins and inhibition of cyclic AMP accumulation.

J. Strnad, C. Eppler, J. Hadcock, 1994, Molecular pharmacology.

Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.

D. Scott, P. Iredale, R. L. Dow, 2012, ACS medicinal chemistry letters.

Role of opiates and their receptors in the regulation of food intake and body weight

D. Scott, J. Hadcock, 2005 .

Discovery and development of next generation sGC stimulators with diverse multidimensional pharmacology and broad therapeutic potential.

J. Masferrer, A. Profy, Emmanuel S. Buys, 2018, Nitric oxide : biology and chemistry.

Blockade of Cannabinoid Type 1 Receptors Augments the Antiparkinsonian Action of Levodopa without Affecting Dyskinesias in 1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine-Treated Rhesus Monkeys

F. Menniti, S. Factor, P. Iredale, 2007, Journal of Pharmacology and Experimental Therapeutics.

Discovery of potent and orally bioavailable heterocycle-based beta3-adrenergic receptor agonists, potential therapeutics for the treatment of obesity.

T. Maurer, D. Hargrove, D. Tess, 2007, Bioorganic & medicinal chemistry letters.

[10] Somatostatin receptor coupling to G proteins

J. Strnad, J. Hadcock, 1996 .

Functional coupling of a mammalian somatostatin receptor to the yeast pheromone response pathway

B. Ozenberger, M. Pausch, J. Hadcock, 1995, Molecular and cellular biology.

Cross-regulation between G-protein-mediated pathways. Activation of the inhibitory pathway of adenylylcylclase increases the expression of beta 2-adrenergic receptors.

J. Port, C. Malbon, J. Hadcock, 1991, The Journal of biological chemistry.

The rat SSTR2 somatostatin receptor subtype is coupled to inhibition of cyclic AMP accumulation.

J. Strnad, C. Eppler, J. Hadcock, 1993, Biochemical and biophysical research communications.

Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles.

D. Scott, P. Iredale, R. L. Dow, 2009, Bioorganic & medicinal chemistry letters.

G protein-coupled receptor 21 deletion improves insulin sensitivity in diet-induced obese mice.

Miriam Scadeng, Da Young Oh, T. Bártfai, 2012, The Journal of clinical investigation.

Beneficial Metabolic Effects of Praliciguat, a Soluble Guanylate Cyclase Stimulator, in a Mouse Diet-Induced Obesity Model

Courtney M. Shea, Emmanuel S. Buys, E. Buys, 2022, Frontiers in Pharmacology.

The CNS-Penetrant Soluble Guanylate Cyclase Stimulator CY6463 Reveals its Therapeutic Potential in Neurodegenerative Diseases

M. Currie, C. Winrow, P. Renhowe, 2021, Frontiers in Pharmacology.

Optimization of triazole -based TGR5 agonists towards orally available agents

Bryan M. Li, J. Warmus, D. Hepworth, 2013 .

Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.

Margaret S. Landis, D. Scott, P. Iredale, 2009, Journal of medicinal chemistry.

Effects of alpha2-adrenoceptor antagonists on metabolic processes of swine: I. Effects on nonesterified fatty acid and plasma urea nitrogen concentrations in jugularly catheterized pigs.

M. Pausch, D. Search, J. Ingling, 1998, Journal of animal science.

Postnatal PPARδ Activation and Myostatin Inhibition Exert Distinct yet Complimentary Effects on the Metabolic Profile of Obese Insulin-Resistant Mice

M. Kuhn, N. LeBrasseur, K. M. Judkins, 2010, PloS one.

Insulin Causes Hyperthermia by Direct Inhibition of Warm-Sensitive Neurons

J. Eberwine, T. Bártfai, H. Kolb, 2009, Diabetes.

Pharmacokinetic/Pharmacodynamic Modeling of a Cell-Penetrating Peptide Phosphorodiamidate Morpholino Oligomer in mdx Mice

Mohammad Shadid, Huadong Sun, J. Hadcock, 2021, Pharmaceutical Research.

Blockade of Cannabinoid CB 1 Receptors Augments the Antiparkinsonian Action of Levodopa without Affecting Dyskinesias in MPTP-Treated Rhesus Monkeys

F. Menniti, S. Factor, P. Iredale, 2007 .

TISSUE-SPECIFIC REGULATION OF α1B, β1 AND β2-ADRENERGIC RECEPTOR mRNAs BY THYROID STATE IN THE RAT

C. Malbon, G. Kunos, J. Hadcock, 1991 .

A single amino acid substitution in somatostatin receptor subtype 5 increases affinity for somatostatin-14.

B. Ozenberger, J. Hadcock, 1995, Molecular pharmacology.

Glucocorticoids down-regulate beta 1-adrenergic-receptor expression by suppressing transcription of the receptor gene.

J. Kíely, C. Malbon, S. Bahouth, 1994, The Biochemical journal.

Evaluation of a Mathematical Model of Rat Body Weight Regulation in Application to Caloric Restriction and Drug Treatment Studies

Jangir Selimkhanov, T. Maurer, D. Scott, 2016, PloS one.

A Selective Cannabinoid-1 Receptor Antagonist, PF-95453, Reduces Body Weight and Body Fat to a Greater Extent than Pair-Fed Controls in Obese Monkeys

K. Kavanagh, J. Hadcock, Li Zhang, 2010, Journal of Pharmacology and Experimental Therapeutics.

The biology of beta-adrenergic receptors: analysis in human epidermoid carcinoma A431 cells.

C. Malbon, H. Wang, M. Berrios, 1991, The International journal of biochemistry.

Down-regulation of beta-adrenergic receptors: agonist-induced reduction in receptor mRNA levels.

C. Malbon, C C Malbon, J R Hadcock, 1988, Proceedings of the National Academy of Sciences of the United States of America.

Comparison of pre‐clinical pharmacokinetic (PK) and pharmacodynamic (PD) relationships of cannabinoid CB1 receptor antagonists in a drug development program for weight loss (WL) management

D. Scott, J. Hadcock, S. Black, 2008 .