Endocannabinoid System Overview

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Questions and Answers

Which of the following receptors is primarily located in the central nervous system?

  • FAAH
  • CB1 (correct)
  • MGL
  • CB2

Endocannabinoids are synthesized and stored in vesicles until needed.

False (B)

What is the primary psychoactive compound found in cannabis?

Delta-9-tetrahydrocannabinol (THC)

Cannabis sativa is known for having approximately _____ active compounds.

<p>400</p> Signup and view all the answers

Match the following endocannabinoid compounds with their functions:

<p>Anandamide = Breaks down by FAAH 2-AG = Breaks down by MGL FAAH = Inactivates anandamide MGL = Inactivates 2-AG</p> Signup and view all the answers

What year was the first receptor for THC (CB1) identified?

<p>1988 (B)</p> Signup and view all the answers

Cannabinoid antagonists can be used to suppress appetite.

<p>True (A)</p> Signup and view all the answers

Which compound was identified as inactive in urine tests for THC?

<p>carboxy-THC</p> Signup and view all the answers

The primary role of endocannabinoids in synaptic transmission is to inhibit the release of __________ from the presynaptic neuron.

<p>neurotransmitter</p> Signup and view all the answers

Which of the following conditions is THC particularly effective for pain relief?

<p>Pain associated with inflammatory conditions (D)</p> Signup and view all the answers

Flashcards

Endocannabinoids

Lipid molecules produced by the body that bind to cannabinoid receptors.

CB1 receptor

Cannabinoid receptor primarily located in the central nervous system (brain and spinal cord).

CB2 receptor

Cannabinoid receptor primarily located in the periphery, including the immune system.

Anandamide

An endocannabinoid broken down by FAAH (fatty acid amide hydrolase).

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2-AG

An endocannabinoid broken down by MGL (monoacylglycerol lipase).

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THC

Psychoactive compound found in cannabis, impacting the brain.

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CBD

Non-psychoactive compound found in cannabis.

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Analgesia

Pain relief, often associated with the ECS and cannabis.

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Synaptic Transmission

Communication between neurons, often influenced by endocannabinoids.

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Retrograde signaling

Endocannabinoids act as messengers from the postsynaptic neuron to the presynaptic neuron.

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Study Notes

Endocannabinoid System

  • Endocannabinoids: Lipid-soluble signaling molecules, not stored in vesicles, synthesized on demand.

  • Functions:

    • Analgesia
    • Sensory processing
    • Motor coordination
    • Memory and cognition
    • Appetite regulation
    • Immune system modulation

  • Synthesis: Derived from arachidonic acid.

  • Receptors:

    • CB1: Primarily in the central nervous system (CNS), involved in motor coordination, memory, and sensory processing. Located in basal ganglia, cerebellum, hippocampus, and cortex. Few in brainstem.
    • CB2: Primarily in the periphery, including the immune system.

  • Inactivation:

    • Anandamide: Broken down by fatty acid amide hydrolase (FAAH) in postsynaptic neurons.
    • 2-AG: Broken down by monoacylglycerol lipase (MGL) in presynaptic neurons.

  • Synaptic Transmission:

    • Postsynaptic neuron depolarization triggers endocannabinoid release.
    • Endocannabinoids diffuse to presynaptic neurons, binding receptors and inhibiting neurotransmitter release (retrograde signaling).

Cannabis

  • Plant: Cannabis sativa and Cannabis indica, cultivated for ~6000 years, originally from Asia, now worldwide.

  • Compounds:

    • Varying compounds; ~400 active compounds,
    • Psychoactive: Delta-9-tetrahydrocannabinol (THC). Identifed in 1964.
    • Non-psychoactive: Cannabidiol (CBD), Cannabinol (CBN).

  • Timeline:

    • 1964: THC identified as active component of marijuana.
    • 1988: First THC receptor (CB1) identified.
    • 1991: Second THC receptor (CB2) identified,
    • 1992: Endogenous THC (anandamide & 2-AG) identified.

  • Pharmacokinetics of THC:

    • Half-life: ~30 hours.
    • Depot binding: "reverse tolerance".
    • Metablism: Metabolized in liver to active metabolite (11-hydroxy-delta-9 THC); then into inactive metabolite (carboxy-THC; detectable in urine).

  • Medical Uses of THC:

    • Analgesia: Sativex (THC + CBD); effective for inflammatory pain (CB2 action).
    • Appetite stimulation: Marinol. Useful in cancer/AIDS.
    • Cannabinoid antagonists can suppress appetite. One example is Rimonabant (2006).

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