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Related Concept Videos

G Protein-coupled Receptors01:15

G Protein-coupled Receptors

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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...
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Opioid Receptors: Overview01:22

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Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...
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CNS Stimulants: Cocaine, Amphetamines and Cannabinoids01:24

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CNS stimulants, such as cocaine, amphetamines, and cannabinoids, have varying structures and mechanisms of action that lead to different therapeutic effects and side effects. Cocaine, with its molecular formula C17H21NO4, is a tropane alkaloid and a tertiary amino compound. It has two chemical forms: the hydrochloride salt and the "freebase." The former is in powder form, while the latter involves removing the hydrochloride salt to create a form that can be smoked. Cocaine exerts its...
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The Two-State Receptor Model01:29

The Two-State Receptor Model

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
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Transducer Mechanism: G Protein–Coupled Receptors01:30

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
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Olfactory Receptors: Location and Structure01:03

Olfactory Receptors: Location and Structure

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The process of olfaction, also known as the sense of smell, is a sophisticated chemical response system. The specialized sensory neurons that facilitate this process, known as olfactory receptor neurons, are situated in an upper segment of the nasal cavity, known as the olfactory epithelium. Olfactory sensory neurons are bipolar, with their dendrites extending from the epithelium's apex into the mucus that lines the nasal cavity. Airborne molecules, when inhaled, traverse the olfactory...
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Oromucosal as an Alternative Method for Administration of Cannabis Products in Rodents
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Structural and Functional Insights into Cannabinoid Receptors.

Xiaoting Li1, Ling Shen2, Tian Hua1

  • 1iHuman Institute, ShanghaiTech University, Shanghai 201210, China.

Trends in Pharmacological Sciences
|August 3, 2020
PubMed
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Understanding cannabinoid receptors (CB1 and CB2) and their interactions is key for developing new drugs. Recent structural insights into these receptors and their signaling pathways pave the way for advanced therapeutic strategies targeting the endocannabinoid system.

Keywords:
G-protein-coupled receptoractivationcannabinoid receptorsendocannabinoid systemsignalingtherapeutic applications

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Area of Science:

  • Pharmacology
  • Molecular Biology
  • Neuroscience

Background:

  • Cannabinoid receptors type 1 (CB1) and 2 (CB2) are crucial targets for treating central nervous system and immune system disorders.
  • The endocannabinoid system (ECS) plays a vital role in physiological functions.
  • Ligand-receptor interactions within the ECS are complex and require detailed study.

Purpose of the Study:

  • To provide an overview of the structural features of cannabinoid receptors.
  • To discuss diverse ligand binding modes.
  • To explore future therapeutic strategies for the endocannabinoid system.

Main Methods:

  • Structural elucidation of cannabinoid receptors and G protein signaling complexes.
  • Analysis of ligand-receptor interactions.
  • Review of current literature on cannabinoid receptor function and therapeutic applications.

Main Results:

  • Breakthroughs in structural biology provide a molecular basis for understanding cannabinoid receptor activation.
  • Detailed insights into ligand binding modes are now available.
  • The structural information facilitates next-generation drug design.

Conclusions:

  • Precise modulation of the endocannabinoid system is achievable through advanced drug design.
  • Understanding receptor structure is critical for developing targeted therapies.
  • Future strategies for therapeutic applications targeting the ECS are discussed.