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Lecture 20 (Cannabis Receptors (CB Receptors) (primary agonist is…

- - - - exists in high concentrations in the brain.
        
        especially in regions association with the limbic system ─ basal ganglia, hypothalamus, amygdala, hippocampus.
      - activation causes psychoactive effects
        
        euphoria
        
        anxiety
        
        appetite stimulation
        
        relaxation
        
        hallucinations
      - Both the analgesic and psychoacive effects are linked to this receptor.
    - - found around the visceral areas of the body, such as the spleen and pancreas
      - found in glial cells and the brainstem
- - - - activation of cell signalling.
  - - - phosphorylation of tyrosines on signalling molecules.
        
        activation of cell signalling.
  - - - ligands are typically classical neurotransmitters
    - - depolarisation
        : increase from RMP.
      - hyperpolarisation
        : decrease from RMP.
- - - - loss of coordination
      - memory loss
      - slurred speech
      - cognitive and behavioural impairments
    - - lower doses associated w/:
        ● loss of inhibitions
        ● relaxation
      - too much may lead to coma or death ─ overactivation of chloride channels.
  - - - has an intrinsic chloride channel.
      - main effects are inhibitory.
      - has many ligands including benzodiazepines, barbiturates, and alcohol.
        
        all examples of substances that produce an inhibitory physiological effect or response to the environment.
- - - - ④ G-protein is activated ─ subunits disssociate into Gα and βγ.
      - ⑤ The dissociated subunits respectively bind to different downstream effectors.
      - ③ GDP bound to the Gα-subunit replaced by high-energy GTP.
      - ② Agonist binds to the receptor.
      - ① Receptor in resting state ─ G-protein is intact and bound to transmembrane receptor.
      - ⑥ A cellular response is generated ─ shorly after, GTP is replaced by GDP.
      - ⑦ The trimer reassembles, then binds to the membrane receptor to restore resting state.