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Membrane Biology > The Cannabinoids > Flashcards

The Cannabinoids Flashcards

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1
Q

Define cannabinoid.

A

All substances capable of activating cannabinoid receptors

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2
Q

What are the 3 main pharma coactive constituents?

A

THC
CBD
CBN

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3
Q

What are the 3 classes of cannabinoids?

A

Endocannabinoids
Phytocannabinoids
Synthetic

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4
Q

What are the 3 endocannabinoid receptors?

A

CB1
CB2
GPR55

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5
Q

Where is CB1 found?

A

Mostly neuronal

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6
Q

Where is CB2 found?

A

Immune cells
new research suggests neuronal function

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7
Q

What are two types of endogenous ligands?

A

Anandamide and 2-AG

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8
Q

What are the 3 enzymes needed for synthesis?

A

Phospholipase D and C and diacylglycerol lipase (DAGL)

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9
Q

What is the precursor for endocannabinoids?

A

Arachidonic acid

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10
Q

What is the uptake mechanism for endocannabinoids?

A

Anandamide transporter (?)

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11
Q

What enzymes breakdown endocannabinoids?

A

Fatty acid amid hydrolase (FAAH) and monoacylglycerol (MGL)

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12
Q

What triggers production of the endocannabinoids 2AG or AEA?

A

Calcium influx or calcium mobilization in post synaptic cell

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13
Q

What receptor does AEA and 2AG act on?

A

CB1 receptors on presynaptic terminal

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14
Q

What happens after AEA and 2AG bind to CB1?

A

Depress neurotransmitter release thus altering neuronal activity

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15
Q

How are endocannabinoids degraded?

A

Taken up via Cannabinoid transporter and degraded by FAAH

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16
Q

What is an agonist at Cb1 and CB2 receptors?

A

WIN 55,212-2

17
Q

What is an antagonist at CB1?

A

Rimonabant

18
Q

What does CB1 activate?

A

Increases activation of inwardly rectifying K+ channels
Decreases activity of N and P/Q calcium channels which decreases neurotransmitter release

19
Q

What are 5 features of endocannabinoids?

A
  1. Synthesised on demand
  2. Not stored in vesicles
  3. Not released from presynaptic terminals
  4. Not specific
  5. Tonic release of endocannabinoids
20
Q

How do endocannabinoids act backwards?

A

Released from postsynaptic cells and act on presynaptic terminals

21
Q

Where are endocannabinoids metabolized from?

A

Phospholipid cell membrane - highly lipid soluble

22
Q

What is Sativex?

A

Cannabinoid medicine for treatment of spasticity due to multiple sclerosis

23
Q

What are 4 distinct effects produced by cannabimimetic drugs in animals?

A

Rigid immobility
Decreased motor activity
Analgesia
Hypothermia

24
Q

What do endocannabinoids mediate?

A

GABA release
Depolarization-induced Suppression of Inhibition

25
Q

How does GABA inhibition occur?

A

Ca2+ influx into principal pyramidal cell initiates synthesis and release of endocannabinoid that activates Cb1 receptors

26
Q

What is TRPV1 involved in?

A

pain transduction

27
Q

How are cannabinoids kept out of the brain?

A

CB2 agonists target novel receptors and manipulate the endocannabinoid system

Membrane Biology (19 decks)

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