Search Results - "Brackeen, Marcus"
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Assessment of the Antinociceptive, Respiratory-Depressant, and Reinforcing Effects of the Low pK a Fluorinated Fentanyl Analogs, FF3 and NFEPP
Published in Neuropharmacology (01-09-2024)“…Recent studies report that fentanyl analogs with relatively low pK values produce antinociception in rodents without other mu opioid-typical side effects due…”
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2
Assessment of the antinociceptive, respiratory-depressant, and reinforcing effects of the low pKa fluorinated fentanyl analogs, FF3 and NFEPP
Published in Neuropharmacology (01-09-2024)“…Recent studies report that fentanyl analogs with relatively low pKa values produce antinociception in rodents without other mu opioid-typical side effects due…”
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3
Identification of a Potent Human Trace Amine-Associated Receptor 1 Antagonist
Published in ACS chemical neuroscience (06-04-2022)“…Human trace amine-associated receptor subtype 1 (hTAAR1) is a G protein-coupled receptor that has therapeutic potential for multiple diseases, including…”
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4
Evaluation of cannabimimetic effects of selected minor cannabinoids and Terpenoids in mice
Published in Progress in neuro-psychopharmacology & biological psychiatry (08-06-2024)“…The cannabis plant contains several cannabinoids, and many terpenoids that give cannabis its distinctive flavoring and aroma. Δ9-Tetrahydrocannabinol (Δ9-THC)…”
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5
Design and Synthesis of Conformationally Constrained Analogs of 4-(3-Butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as Potent Inhibitors of cAMP-Specific Phosphodiesterase
Published in Journal of medicinal chemistry (01-11-1995)“…The synthesis and biological evaluation of cAMP-specific phosphodiesterase (PDE IV) inhibitors is described. The PDE IV inhibitor…”
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Phosphodiesterase Type IV Inhibition. Structure-Activity Relationships of 1,3-Disubstituted Pyrrolidines
Published in Journal of medicinal chemistry (01-04-1995)“…The synthesis of 1,3-disubstituted pyrrolidines 2 and their activities as type IV phosphodiesterase (PDE) inhibitors are described. Various groups were…”
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Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of methyl (R,R)-(.+-.)-3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3- methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase
Published in Journal of medicinal chemistry (01-12-1995)Get full text
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8
Conformationally Constrained Analogues of N-(Piperidinyl)-5-(4-Chlorophenyl)-1-(2,4- Dichlorophenyl)-4-Methyl-1H-Pyrazole-3-Carboxamide (SR141716): Design, Synthesis, Computational Analysis, And Biological Evaluations
Published in Journal of medicinal chemistry (26-06-2008)“…Structure−activity relationships (SARs) of 1 (SR141716) have been extensively documented, however, the conformational properties of this class have received…”
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N-(2-Benzoylphenyl)-l-tyrosine PPARγ Agonists. 1. Discovery of a Novel Series of Potent Antihyperglycemic and Antihyperlipidemic Agents
Published in Journal of medicinal chemistry (03-12-1998)“…We have identified a novel series of antidiabetic N-(2-benzoylphenyl)-l-tyrosine derivatives which are potent, selective PPARγ agonists. Through the use of in…”
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Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgesics
Published in Journal of medicinal chemistry (01-07-1991)Get full text
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Conformationally Constrained Analogues of N -(Piperidinyl)-5-(4-Chlorophenyl)-1-(2,4- Dichlorophenyl)-4-Methyl-1 H -Pyrazole-3-Carboxamide (SR141716): Design, Synthesis, Computational Analysis, And Biological Evaluations
Published in Journal of medicinal chemistry (01-06-2008)Get full text
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12
Conformational characteristics of the interaction of SR141716A with the CB1 cannabinoid receptor as determined through the use of conformationally constrained analogs
Published in The AAPS journal (27-10-2006)“…Interest in cannabinoid pharmacology increased dramatically upon the identification of the first cannabinoid receptor (CB1) in 1998 and continues to expand as…”
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Design, synthesis, and pharmacological evaluation of ultrashort- to long-acting opioid analgetics
Published in Journal of medicinal chemistry (01-07-1991)“…In an effort to discover a potent ultrashort-acting mu opioid analgetic that is capable of metabolizing to an inactive species independent of hepatic function,…”
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A novel route to the 4-anilido-4-(methoxycarbonyl)piperidine class of analgetics
Published in Journal of organic chemistry (01-06-1990)Get full text
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15
Evaluation of the significance of elevated levels of systemic and localized tumor necrosis factor in different animal models of inflammation
Published in The Journal of laboratory and clinical medicine (01-12-1994)“…Elevated tumor necrosis factor (TNF) levels have been reported in various models of acute and chronic inflammation and used by many investigators to determine…”
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