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Related Concept Videos

Drug-Receptor Interactions01:29

Drug-Receptor Interactions

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Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue....
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The Two-State Receptor Model01:29

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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.
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Drug-Receptor Bonds01:25

Drug-Receptor Bonds

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Drug-receptor bonds are formed through various chemical forces when drugs interact with target cells. Covalent bonds, strong and irreversible, are exemplified by DNA-alkylating anticancer agents that inhibit cell division. However, such irreversible drug binding lacks selectivity and can modify the DNA of the surrounding healthy cells. Covalent binding often contributes to tissue toxicity, as seen with chloroform and paracetamol metabolites binding to the liver, causing hepatotoxicity.
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The Equilibrium Binding Constant and Binding Strength02:18

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The equilibrium binding constant (Kb) quantifies the strength of a protein-ligand interaction. Kb can be calculated as follows when the reaction is at equilibrium:
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Quantitative Aspects of Drug-Receptor Interaction01:30

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The receptor occupancy theory connects a drug's response to the number of occupied receptors. With higher drug concentrations, more receptors are occupied, leading to increased responses. The formation of drug-receptor complexes involves association and dissociation rates, which reach equilibrium when the forward and backward reactions are equal. The equilibrium association constant (Ka) and its inverse, the equilibrium dissociation constant (Kd), indicate drug affinity. Higher Ka and lower...
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Creating Highly Specific Chemically Induced Protein Dimerization Systems by Stepwise Phage Selection of a Combinatorial Single-Domain Antibody Library
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CBD Versus CBDP: Comparing In Vitro Receptor-Binding Activities.

Mehdi Haghdoost1, Scott Young2, Alisha K Holloway3

  • 1Nalu Bio Inc., 38 Keyes Avenue, Suite 117, San Francisco, CA 94129, USA.

International Journal of Molecular Sciences
|July 27, 2024
PubMed
Summary
This summary is machine-generated.

Cannabidiphorol (CBDP) and cannabidiol (CBD) show similar activity, with CBD being a slightly more potent CB2 receptor antagonist. Unexpectedly, CBDP acted as a positive allosteric modulator at mu-opioid receptors, unlike CBD.

Keywords:
agonistantagonistscannabidiolcannabidiphorolcannabinoid receptor

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Area of Science:

  • Pharmacology
  • Biochemistry
  • Molecular Biology

Background:

  • Phytocannabinoids with seven-carbon alkyl chains (phorols), such as cannabidiphorol (CBDP), are gaining attention due to presumed higher potency than shorter-chain analogs.
  • Cannabidiphorol (CBDP) and tetrahydrocannabiphorol (THCP) are commercially available, yet their biological activities remain largely uncharacterized.

Purpose of the Study:

  • To investigate the in vitro receptor-binding activity and relative potency of cannabidiphorol (CBDP) compared to cannabidiol (CBD).
  • To explore the interaction of CBDP with cannabinoid, serotonin, and opioid receptors.

Main Methods:

  • In vitro receptor-binding experiments assessing CBDP's antagonism at CB1/CB2 receptors, agonism at 5HT-1A and dopamine D2S receptors, and modulation at mu-opioid receptors.
  • Radioligand binding assays to identify primary biological targets.
  • Molecular docking simulations to elucidate structural mechanisms of receptor interaction.

Main Results:

  • CBDP and CBD exhibited similar activity profiles, with CBD showing slightly greater potency as a CB2 receptor antagonist (p < 0.05).
  • CB2 receptors were identified as a likely primary target for CBDP, though both cannabinoids were less potent than SR144528.
  • CBDP demonstrated unexpected positive allosteric modulator (PAM) activity at mu-opioid receptors, contrasting with the expected negative allosteric modulator (NAM) effects of cannabidiols.

Conclusions:

  • Contrary to expectations, CBDP is not inherently more potent than CBD and exhibits a distinct interaction profile at the mu-opioid receptor.
  • Molecular docking suggests co-binding of CBDP and met-enkephalin to the mu-opioid receptor, explaining the observed PAM effect.
  • Further research is needed to fully understand the pharmacological implications of CBDP's unique receptor interactions.