86188-25-2

Usage

Uses

Used in Pharmaceutical Industry:
(RS)-1-(thiophen-3-yl)propan-2-amine hydrochloride is used as a psychoactive drug for its stimulant properties, which can increase alertness, attention, and energy levels in individuals. It is utilized in the treatment of certain medical conditions that require stimulation of the central nervous system.
Used as a Performance-Enhancing Drug:
(RS)-1-(thiophen-3-yl)propan-2-amine hydrochloride is used as a performance-enhancing drug due to its ability to increase alertness, attention, and energy levels. This makes it appealing to athletes and individuals seeking to improve their physical or cognitive performance.
Used for Recreational Purposes:
(RS)-1-(thiophen-3-yl)propan-2-amine hydrochloride is also used for recreational purposes because of its stimulating and euphoric effects. However, its use is regulated in many countries due to the potential for abuse and addiction.

Upstream product

• 498-62-4 3-thiophene carboxaldehyde 
• 149977-36-6 (E)-3-(2-nitroprop-1-en-1-yl)thiophene 

Downstream Products

• 1997387-43-5 C₁₉H₂₇N₃O₂S 
• 1997387-43-5 1-[(R)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-((S)-1-(thiophen-3-yl)propan-2-yl)urea 
• 1997387-43-5 1-[(R)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-((R)-1-(thiophen-3-yl)propan-2-yl)urea 
• 1997387-43-5 1-[(S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-((R)-1-(thiophen-3-yl)propan-2-yl)urea 
• 1997387-43-5 1-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea 

Relevant academic research and scientific papers

Synthesis and evaluation of novel biased μ-opioid-receptor (μOR) agonists

‘Biased’ ligands of G protein-coupled receptors (GPCRs) represent a type of promising analgesic with reduced on-target side effects. PZM21, a potent μ-opioid-receptor (μOR)-biased agonist with a new chemical scaffold compared to classic opioids, has been identified as a therapeutic lead molecule for treating pain. In the current study, novel PZM21 analogues were synthesized and evaluated for their in vitro and in vivo efficacy. Novel compound 7a and PZM21 demonstrated undetectable β-arrestin-2 recruitment, however, their analgesic effects need to be further confirmed. Compounds 7b, 7d, and 7g were stronger analgesics than PZM21 in both the mouse formalin injection assay and the writhing test. Compound 7d was the most potent analogue, requiring a dose that was 1/16th to 1/4th of that of PZM21 for its analgesic activity in the two assays, respectively. Therefore, compound 7d could serve as a lead to develop new biased μOR agonists for treating pain.

Biased agonist and medical application thereof

The invention relates to compounds shown in structural formulas I and II, stereoisomers or pharmaceutically acceptable salts thereof, and a pharmaceutical composition containing the compounds, the stereoisomers or the pharmaceutically acceptable salts thereof as active ingredients, and uses of the compound, the stereoisomer thereof or the pharmaceutically acceptable salt thereof in preparation ofanalgesic drugs.

Discovery of Biased Mu-Opioid Receptor Agonists for the Treatment of Pain

G protein-biased mu-opioid receptor (MOR) agonists have been developed as promising new potent analgesic drugs with fewer adverse side effects than standard MOR agonists. PZM21 represents a unique chemotype unrelated to known opioids, which makes it a desirable lead for modification to find analgesics with new chemical entities. In the present study, we synthesized and tested novel PZM21 derivatives as potent biased MOR agonists by introducing a benzodioxolane group to replace the hydroxybenzene of PZM21. The new compounds displayed more potent analgesic activities in vivo and greater bias toward G protein signaling in vitro than did PZM21. These results suggest that the benzodioxolane group is essential for the maintenance of bias. Compounds 7 i ((S)-1-(3-(benzo[d][1,3]dioxol-4-yl)-2-(dimethylamino)propyl)-3-phenethylurea) and 7 j ((S)-1-(3-(benzo[d][1,3]dioxol-4-yl)-2-(dimethylamino)propyl)-3-benzylurea) could serve as new leads for further modifications to find novel biased MOR agonists with greater G protein signaling potency and less β-arrestin-2 recruitment.

MU OPIOID RECEPTOR MODULATORS

Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

Thieno tetrahydropyridines useful as class III antiarrhythmic agents

This invention relates to thieno tetrahydropyridine and isoquinoline derivative compounds which are useful as antiarrhythmic agents, pharmaceutical compositions comprising such compounds, novel intermediates for their preparation and their methods of use. More particularly these thieno tetrahydropyridine and isoquinoline derivative compounds have been demonstrated to increase the effective refractory period (ERP) of isolated perfused cardiac tissue in vitro.