960305-55-9Relevant academic research and scientific papers
Structure-activity relationships of 7-substituted dimethyltyrosine-tetrahydroisoquinoline opioid peptidomimetics
Montgomery, Deanna,Anand, Jessica P.,Baber, Mason A.,Twarozynski, Jack J.,Hartman, Joshua G.,Delong, Lennon J.,Traynor, John R.,Mosberg, Henry I.
, (2019/12/23)
The opioid receptors modulate a variety of biological functions, including pain, mood, and reward. As a result, opioid ligands are being explored as potential therapeutics for a variety of indications. Multifunctional opioid ligands, which act simultaneously at more than one type of opioid receptor, show promise for use in the treatment of addiction, pain, and other conditions. Previously, we reported the creation of bifunctional kappa opioid receptor (KOR) agonist/mu opioid receptor (MOR) partial agonist ligands from the classically delta opioid receptor (DOR) antagonist selective dimethyltyrosine-tetrahydroisoquinoline (Dmt-Tiq) scaffold through the addition of a 7-benzyl pendant on the tetrahydroisoquinoline ring. This study further explores the structure-activity relationships surrounding 7-position pendants on the Dmt-Tiq scaffold. Some analogues maintain a KOR agonist/MOR partial agonist profile, which is being explored in the development of a treatment for cocaine addiction. Others display a MOR agonist/DOR antagonist profile, which has potential to be used in the creation of a less addictive pain medication. Ultimately, we report the synthesis and in vitro evaluation of novel opioid ligands with a variety of multifunctional profiles.
Novel Dimethyltyrosine-Tetrahydroisoquinoline Peptidomimetics with Aromatic Tetrahydroisoquinoline Substitutions Show in Vitro Kappa and Mu Opioid Receptor Agonism
Montgomery, Deanna,Anand, Jessica P.,Griggs, Nicholas W.,Fernandez, Thomas J.,Hartman, Joshua G.,Sánchez-Santiago, Ashley A.,Pogozheva, Irina D.,Traynor, John R.,Mosberg, Henry I.
, p. 3682 - 3689 (2019/09/10)
The dimethyltyrosine-tetrahydroisoquinoline (Dmt-Tiq) scaffold was originally developed in the production of selective delta opioid receptor (DOR) antagonists. Installation of a 7-benzyl pendant on the tetrahydroisoquinoline core of this classic opioid scaffold introduced kappa opioid receptor (KOR) agonism. Further modification of this pendant resulted in retention of KOR agonism and the addition of mu opioid receptor (MOR) partial agonism, a bifunctional profile with potential to be used in the treatment of cocaine addiction.
PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY
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Page/Page column 77-78, (2012/03/09)
The present invention relates to phenalkylamine derivatives of the formula (I) or (II); or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phena
AMIDINE DERIVATIVE
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Page/Page column 22, (2011/05/04)
Provision of a novel amidine derivative or a pharmaceutically acceptable salt thereof having an activated blood coagulation factor X-inhibitory activity. A compound represented by the formula (I) wherein each symbol is as defined above, or a pharmaceutically acceptable salt thereof.
FUSED HETEROCYCLIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 19; 34-35, (2010/05/13)
The present invention is directed to fused heterocyclic compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schi
