Lecture 12 Eicosanoids & Cannabinoids Flashcards

1
Q

What do Eicosanoids do?

A

Play an important role in inflammation

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2
Q

Eicosanoids are generated from what?

A

Arachidonic Acid (Fatty Acid Precursor)

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3
Q

Prostaglandins

A

Eicosanoid
Prostanoid

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4
Q

Thromboxanes

A

Eicosanoid
Prostanoid

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5
Q

Leukotriene

A

Eicosanoid

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6
Q

Epoxyeicosatrienoic Acid (EET)

A

Eicosanoid

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7
Q

Arachidonic Acid Metabolism (How id AA made?)

A

Phospholipids –> Arachidonic Acid
Converted by Phospholipase A2

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8
Q

Arachidonic Acid Metabolism (What does AA make?)

A

Lipoxygenases (5-lipoxygenase) converts AA –> HPETE
HPETE can be made into Leukotrienes

COX1/COX2 converts AA into Prostanoids

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9
Q

Arachidonic Acid Metabolism (Prostanoids)

A

Depending on the environemnt and what enzymes are around Prostanoids are then converted into prostaglandins
Their are many types of Prostaglandins

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10
Q

Prostacyclin (Metabolism Path)

A

Prostanoid –> Prostacyclin (PGI2)

Initiated by Prostacyclin Synthase in Endothelium

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11
Q

Prostacyclin (Effects)

A

Inhibits Platelet Aggregation
Vasodilator

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12
Q

Thromboxane (Metabolism Path)

A

Prostanoid –> Thromboxane (TXA2)

Initiated by Thromboxane Synthase in Platelets

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13
Q

Thromboxane (Effects)

A

Promotes Platelet Aggregation
Vasoconstriction

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14
Q

PGD2

A

Prostanoid

Vasodilation
Inhibits Platelet Aggregation
Relaxes GI and Uterus Muscles

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15
Q

PGE2

A

Main Inflammatory Prostanoid
Vasodilator
Decrease Blood Flow by heat (Pyrogenic)

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16
Q

PGF(2-alpha)

A

Uterine Contractions

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17
Q

Alprostadil

A

PGE1

Vasodilation

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18
Q

Misoprostol

A

PGE2

Inhibits Gastric Acid secretion
Stimulates GI Muscous secretion

Uterine Contractions (Terminates Early Pregnancy)
Cervical Ripening/Dilation (Induce Labour)

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19
Q

Gemeprost

A

PGE2

Uterine Contractions (Terminates Early Pregnancy)

20
Q

Dinoprostone

A

PGE2

Cervical Ripening/Dilation (Induce Labour)

21
Q

Carboprost

A

PGF2-alpha

Uterine Contraction (Uses blood to cause)

22
Q

Latanoprost

A

PGF2-alpha

Uterine Contraction

Also contracts eye to release fluid

23
Q

Epoprostenol

A

PGI2

Inhibits Platelet Aggregation
Vasodilator (Treats Hypertension)

24
Q

What are Leukotrienes made by?

A

White Blood Cells from arachidonic acid

25
What are the two receptor types for Leukotrienes
BLT CysLT
26
LTB4
Binds to BLT receptors Pro-inflammatory leukotriene Stimulates neutrophil chemotaxis Stimulates proliferation and cytokine production By Macrophages and Lymphocytes
27
Cysteinyl Leukotrienes
Binds to CysLT Receptors Contract Bronchi Muscles Contracts cornea Vasodilation in most other vessels
28
Zafirlukast
CysLT Receptor Antagonist Treats Asthma (Prevents Bronchi Constriction)
29
Montelukast
CysLT Receptor Antagonist Treats Asthma (Prevents Bronchi Constriction)
30
THC (Tetrahydrocannabinol)
Main psychoactive compound in Cannabis
31
CBD (Cannabinoid)
Non psychoactive compound in Cannabis, has some medicinal effects
32
Subjective Effects of THC
Relaxation Sharpened Sensory Mimics Psychosis
33
Objective Effects of THC
Increased Hunger Impaired Motor Skills Impaired Short-Term Memory Antiemetic Analgesia Catalepsy
34
Peripheral Effects of THC
Vasodilation (More in the eyes) Bronchodilation Decreased Intraocular Pressure
35
Cannabinoid Receptor Types What kind of receptors are they?
CB1 and CB2 Both are G-Protein (Gi or G0) Inhibits AC Inhibit voltage gated Ca2+ Channels Hyperpolarization
36
CB1 (Where)
Brain Pre-Synaptic and inhibit transmitter release Endothelial cells, adipocytes, peripheral nerves
37
CB2 (Where)
Immune Cells
38
When is COX-1 active
Constitutive (Active all the time)
39
When is COX-2 active
Inducible (Activated by certain conditions)
40
Endocannabinoids
Natural cannabinoids made in the body from phospholipids Retrograde Mediators (Signals from Postsynaptic --> Presynaptic)
41
Anandamide
Endocannabinoid
42
2-arachidonyl glycerol
Endocannabinoid
43
Endocannabinoids (Neuromodulatory Actions)
Nociception Cardiovascular, GI, Respiratory Function Food Intake/Appetite Reproductive Function
44
Nabiximols
CB Agonist Mix of THC & CBD Treats Pain
45
Nabilone
Synthetic Cannabinoid Treats Nausea and Vomitting associated with Chemotherapy
46