Synthesis of Sigma-1 Receptor Ligands

Primary Faculty Mentor’s Name

Karla-Sue Marriott

Proposal Track

Student

Session Format

Poster

Abstract

There are two different types of sigma receptors located throughout the human body; these receptors are sigma-1 and sigma-2 receptors. In scientific history, sigma-1 receptors have received the most attention in comparison to sigma-2 receptors that yield great difficulty in cloning. Sigma-1 receptors are endoplasmic reticulum protein, which makes the receptor profound through the body both centrally and peripherally. In previous research, sigma-1 receptors have acted as binding sites for various drugs that act as ligands. Pharmaceuticals such as, neuroactive steroids, neuroleptics, and antipsychotics. Sigma-1 receptors can function as a modulator for dopamine, acetylcholine, N-Methyl-D-aspartate (NMDA), and opioid receptors. Novel ligands can be developed selective for the sigma-1 receptor using the Perkin base rearrangement reaction and a modified Finkelstein halogen-exchange. Sigma-1 receptor ligands developed in the lab will therefore have the possibility in treating neurodegenerative disorders such as Parkinson’s and Alzheimer's, and possibly even the treatment of cancer. The current engagement on the synthesis of amide derivatives of benzofuran carboxylic acids are to produce ligands that can bind selectively to the sigma-1 receptor. Continued work for analyzing sigma-1 receptor ligands are GC/MS, NMR, and thin-layer chromatography to determine values for these novel ligands.

Award Consideration

1

Location

Concourse/Atrium

Presentation Year

2014

Start Date

11-15-2014 2:55 PM

End Date

11-15-2014 4:10 PM

Publication Type and Release Option

Presentation (Open Access)

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Nov 15th, 2:55 PM Nov 15th, 4:10 PM

Synthesis of Sigma-1 Receptor Ligands

Concourse/Atrium

There are two different types of sigma receptors located throughout the human body; these receptors are sigma-1 and sigma-2 receptors. In scientific history, sigma-1 receptors have received the most attention in comparison to sigma-2 receptors that yield great difficulty in cloning. Sigma-1 receptors are endoplasmic reticulum protein, which makes the receptor profound through the body both centrally and peripherally. In previous research, sigma-1 receptors have acted as binding sites for various drugs that act as ligands. Pharmaceuticals such as, neuroactive steroids, neuroleptics, and antipsychotics. Sigma-1 receptors can function as a modulator for dopamine, acetylcholine, N-Methyl-D-aspartate (NMDA), and opioid receptors. Novel ligands can be developed selective for the sigma-1 receptor using the Perkin base rearrangement reaction and a modified Finkelstein halogen-exchange. Sigma-1 receptor ligands developed in the lab will therefore have the possibility in treating neurodegenerative disorders such as Parkinson’s and Alzheimer's, and possibly even the treatment of cancer. The current engagement on the synthesis of amide derivatives of benzofuran carboxylic acids are to produce ligands that can bind selectively to the sigma-1 receptor. Continued work for analyzing sigma-1 receptor ligands are GC/MS, NMR, and thin-layer chromatography to determine values for these novel ligands.