827017-71-0Relevant academic research and scientific papers
Synthesis and evaluation of novel, selective, functionalized γ-butyrolactones as sigma-2 ligands
Blass, Benjamin E.,Blattner, Kevin M.,Canney, Daniel J.,Gao, Rong,Gordon, John C.,Pippin, Douglas A.
, p. 337 - 349 (2022/01/19)
The sigma-2 (σ2) receptor was discovered nearly 40 years ago and was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein)). Aberrant σ2 activity has been linked to diseases
Design, synthesis, and evaluation of novel, selective γ-butyrolactones sigma-2 ligands
Blass, Benjamin E.,Blattner, Kevin M.,Canney, Daniel J.,Gao, Rong,Gordon, John C.,Pippin, Douglas A.
, p. 1713 - 1727 (2021/08/03)
Nearly 40 years after the first disclosure of sigma receptors, the sigma-2 (σ2) receptor was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein). This macromolecule has been associated with a nu
NOVEL MODULATORS OF THE SIGMA-2 RECEPTOR AND THEIR METHOD OF USE
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Paragraph 0539; 0541, (2018/10/19)
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma- 2 receptor activity.
5-HYDROXYTRYPTAMINE RECEPTOR 7 MODULATORS AND THEIR USE AS THERAPEUTIC AGENTS
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Paragraph 0487; 0489, (2018/10/19)
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
NOVEL 5-HYDROXYTRYPTAMINE RECEPTOR 7 ACTIVITY MODULATORS AND THEIR METHOD OF USE
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Paragraph 0247; 0248; 0249, (2016/06/01)
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
NOVEL SIGMA-2 RECEPTOR BINDERS AND THEIR METHOD OF USE
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Paragraph 307; 309, (2016/11/28)
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.
Homologation as a lead modification approach en route to a series of lactone-based muscarinic ligands
Gao, Rong,Bhandare, Richie R.,Canney, Daniel J.
, p. 1023 - 1030 (2014/03/21)
Previous work identified the lactone ring as a useful scaffold for the design of muscarinic ligands and reported a lactone-based ligand with an IC 50 of 340 nM. Using homologation as a lead modification approach, a new series of lactone-based c
NOVEL 5-HYDROXYTRYPTAMINE RECEPTOR 7 ACTIVITY MODULATORS AND THEIR METHOD OF USE
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Paragraph 0270; 0271; 0272, (2014/10/18)
Pharmaceiiticai compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
Synthesis and evaluation of 5-substituted derivatives of 4,5-dihydro-3,3-diethyl-2(3H)-furanone as subtype-selective muscarinic leads
Ahungena, Alemayyehu,Gabriel, Jerome L.,Canney, Daniel J.
, p. 481 - 511 (2007/10/03)
A series of 5-substituted 4,5 dihydro-3,3-diethyl-2(3H)-furanones were prepared and evaluated as ligands for cholinergic receptors. 3,3-Diethyl-5-imidazolylmethyl-2(3H)-furanone (12), showed a three-fold selectivity for the M2 receptor subtype
