scholarly journals Convergent synthesis of 2-thioether-substituted (N)-methanocarba-adenosines as purine receptor agonists

RSC Advances ◽  
2021 ◽  
Vol 11 (44) ◽  
pp. 27369-27380
Author(s):  
R. Rama Suresh ◽  
Russell B. Poe ◽  
Baorui Lin ◽  
Kexin Lv ◽  
Ryan G. Campbell ◽  
...  
Keyword(s):  
Purinergic Receptor ◽  
Efficient Synthesis ◽  
Receptor Ligands ◽  
Convergent Synthesis ◽  
Receptor Agonists ◽  
Nucleotides And Nucleosides ◽  
Purine Receptor

Enabling efficient synthesis of rigid methanocarba nucleotides and nucleosides as clinically promising purinergic receptor ligands.

Efficient Synthesis of Heterocyclic Neurotensin Receptor Ligands by Microwave-Assisted Aminocarbonylation

Synthesis ◽  
2013 ◽  
Vol 45 (17) ◽  
pp. 2474-2480 ◽  
Author(s):  
Peter Gmeiner ◽  
Christopher Lang
Keyword(s):  
Efficient Synthesis ◽  
Receptor Ligands ◽  
Microwave Assisted ◽  
Neurotensin Receptor

Lactams as Prostanoid Receptor Ligands. Part 4. 2-Piperidones as Selective EP4 Receptor Agonists.

ChemInform ◽  
2005 ◽  
Vol 36 (38) ◽  
Author(s):  
Todd R. Elworthy ◽  
Emma R. Brill ◽  
Christopher C. Caires ◽  
Woongki Kim ◽  
Leang K. Lach ◽  
...  
Keyword(s):  
Receptor Ligands ◽  
Prostanoid Receptor ◽  
Receptor Agonists ◽  
Ep4 Receptor

scholarly journals N-Phenethyl Substitution in 14-Methoxy-N-methylmorphinan-6-ones Turns Selective µ Opioid Receptor Ligands into Dual µ/δ Opioid Receptor Agonists

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Maria Dumitrascuta ◽  
Marcel Bermudez ◽  
Tanila Ben Haddou ◽  
Elena Guerrieri ◽  
Lea Schläfer ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Ligands ◽  
Receptor Agonists ◽  
Opioid Receptor Ligands ◽  
Δ Opioid Receptor ◽  
Opioid Receptor Agonists

Calcium-dependent release of arachidonic acid in response to purinergic receptor activation in airway epithelium

1994 ◽  
Vol 266 (2) ◽  
pp. C406-C415 ◽  
Author(s):  
E. R. Lazarowski ◽  
R. C. Boucher ◽  
T. K. Harden
Keyword(s):  
Arachidonic Acid ◽  
Inositol Phosphate ◽  
Purinergic Receptor ◽  
Receptor Activation ◽  
Normal Donor ◽  
Maximal Effect ◽  
Airway Epithelial ◽  
Arachidonic Acid Release ◽  
Receptor Agonists ◽  
Acid Release

The effect of purinergic receptor agonists on arachidonic acid release was investigated in [3H]arachidonic acid-prelabeled human airway epithelial cells. Exposure of bronchial epithelial BEAS39 cells to extracellular ATP resulted in a marked release of unesterified [3H]arachidonic acid with maximal effect observed within 60-90 s. [3H]diacylglycerol and [3H]phosphatidic acid accumulated in parallel with [3H]arachidonic acid. ATP-stimulated [3H]arachidonic acid release with a K0.5 of 9 +/- 2 microM and UTP was equipotent; no effect was observed with P2Y- or P2X-purinergic receptor agonists or with adenosine. Similar results were obtained with primary cultures of normal human nasal epithelium, CF/T43 and HBE1 airway epithelial cell lines derived from a cystic fibrosis patient and from a normal donor, respectively, and HT-29 human colon carcinoma cells. ATP stimulated inositol phosphate formation in BEAS39 cells with a concentration dependence identical to that for [3H]arachidonic acid release. The effect of ATP on both [3H]arachidonic acid release and inositol phosphate formation was equally inhibited by pertussis toxin. The Ca2+ ionophore A-23187 mimicked the effects of ATP or UTP on arachidonic acid release, and a marked inhibitory effect was observed with thapsigargin. The protein kinase C inhibitor staurosporine partially inhibited ATP-stimulated [3H]arachidonic acid release. These data are consistent with the hypothesis that phospholipase A2 activation is secondary to P2U-purinergic receptor stimulation of D-myoinositol 1,4,5-trisphosphate production and calcium mobilization from intracellular stores.

P2X purinergic receptor ligands: recently patented compounds

2010 ◽  
Vol 20 (5) ◽  
pp. 625-646 ◽  
Author(s):  
Hendra Gunosewoyo ◽  
Michael Kassiou
Keyword(s):  
Purinergic Receptor ◽  
Receptor Ligands

Efficient synthesis of the optically active dihydropyrimidinone of a potent α1A- selective adrenoceptor antagonist

2002 ◽  
Vol 80 (6) ◽  
pp. 646-652 ◽  
Author(s):  
Daniel R Sidler ◽  
Nancy Barta ◽  
Wenjie Li ◽  
Essa Hu ◽  
Louis Matty ◽  
...  
Keyword(s):  
Coupling Reaction ◽  
Optically Active ◽  
Efficient Synthesis ◽  
Enzymatic Resolution ◽  
Convergent Synthesis ◽  
Adrenoceptor Antagonist ◽  
Salient Features ◽  
Palladium Coupling

The convergent synthesis of a potent α1A-selective adrenoceptor antagonist is described. Salient features of the synthesis include the enzymatic resolution of a racemic dihydropyrimidinone and the use of a palladium coupling reaction in the synthesis of 2,4'-dipyridyl.Key words: dihydropyrimidinone, enzymatic resolution, palladium coupling.

Purinergic Receptor Ligands Stimulate Pro-Opiomelanocortin Gene Expression in AtT-20 Pituitary Corticotroph Cells

2006 ◽  
Vol 18 (4) ◽  
pp. 273-278 ◽  
Author(s):  
L.-F. Zhao ◽  
Y. Iwasaki ◽  
Y. Oki ◽  
M. Tsugita ◽  
T. Taguchi ◽  
...  
Keyword(s):  
Gene Expression ◽  
Purinergic Receptor ◽  
Receptor Ligands

Inhibitory, facilitatory, and excitatory effects of ATP and purinergic receptor agonists on the activity of rat cutaneous nociceptors in vitro

2005 ◽  
Vol 51 (4) ◽  
pp. 405-416 ◽  
Author(s):  
Hiroki Yajima ◽  
Jun Sato ◽  
Rocio Giron ◽  
Ryogo Nakamura ◽  
Kazue Mizumura
Keyword(s):  
Purinergic Receptor ◽  
Receptor Agonists
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