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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
Structure-Activity Relationships and Drug Design01:28

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...
Drug Regulation01:25

Drug Regulation

Drug regulation encompasses the management of drug usage by evaluating its safety and efficacy through assessments conducted by regulatory authorities. Regrettably, the history of drug regulation is marred by several catastrophic events. One such incident is the Elixir Sulfanilamide tragedy, in which the toxic compound diethyl glycol was included in a sweet-tasting medication, leading to numerous fatalities. This event prompted the enactment of the Food, Drug, and Cosmetic Act in 1938. Under...
G-protein Coupled Receptors01:21

G-protein Coupled Receptors

G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions01:15

Impact of Pharmacokinetic–Pharmacodynamic Models: Regulatory Decisions

PK–PD modeling has significantly influenced FDA regulatory decisions, particularly drug approval, dosage optimization, and labeling. These models integrate pharmacokinetics (PK) and pharmacodynamics (PD) to predict drug behavior and effects, aiding in optimizing dosing regimens and enhancing the probability of clinical trial success.One notable example is Nesiritide (Natrecor®), a recombinant human brain natriuretic peptide for treating acute decompensated congestive heart failure (CHF).

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Characterizing Modulators of Protease-Activated Receptors with a Calcium Mobilization Assay Using a Plate Reader
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Published on: May 24, 2024

Sigma receptor modulators: a patent review.

Simona Collina1, Raffaella Gaggeri, Annamaria Marra

  • 1University of Pavia, Department of Drug Sciences, Medicinal Chemistry and Pharmaceutical Technology Section, Pavia, Italy. simona.collina@unipv.it

Expert Opinion on Therapeutic Patents
|February 8, 2013
PubMed
Summary

Sigma receptor modulators show promise for treating central nervous system disorders like depression and Alzheimer's disease. Research highlights their potential in neuropathic pain and neurodegenerative conditions.

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Area of Science:

  • Pharmacology
  • Neuroscience
  • Medicinal Chemistry

Background:

  • Sigma receptors are implicated in various central nervous system (CNS) disorders, including mood disorders, psychosis, movement disorders, and memory deficits.
  • Emerging research indicates sigma receptor involvement in neuropathic pain and cancer.

Purpose of the Study:

  • To review advancements in sigma receptor modulator research from 1986 to 2012, focusing on patent literature.
  • To analyze the evolution of sigma receptor modulators and their applications in CNS diseases, neuropathic pain, and neurodegenerative pathologies.

Main Methods:

  • Comprehensive literature search of patent databases (Espacenet, Orbit, ISI Web) and PubMed.
  • Categorization of patents by time frame and applicant.
  • Focus on the development and application trends of sigma receptor modulators.

Main Results:

  • Significant progress in understanding sigma receptor biology and pharmacology.
  • Identification of several sigma receptor modulators with therapeutic potential.

Conclusions:

  • Increased research interest in sigma modulators for diverse pathologies due to biological advancements.
  • Limited number of potent sigma receptor agonists and antagonists (SA4503, ANAVEX 2-73, E-52862) currently in clinical trials for neurodegenerative diseases and neuropathic pain.