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Caffeine base
purinergic
adenosine A1
normally inhibitory, stops adenylyl cyclase. Found in reward and hippocampus
adenosine A2
normally excitatory, starts adenylyl cyclase, found in DA rich regions on GABA neurons
caffeine reward
adenosine A1 receptor on DA neuron’s disinhibiting them
Paraxanthine
Caffeine metabolite, increases blood glycerol and fatty acids via lipolysis
Theobromine
Caffeine metabolite, dilates vessels (periphery) and increases urine
theophylline
caffeine metabolite, inhibits PDE increasing cAMP is the increased breathing mechanism
Nootropics
cognitive enhancers (BDNF linked to LTP in hippocampus)
-caffeine
-taurine
-nicotine
-ritalin
-afinil family
-l-theane
- ginko and ginseng
-amphetamines
Nicotine base
Alkaloid, want it in free base form so burn it
Diacetyl
butter flavour destories lungs
vit E acetate
in vapes causes allergic reactions
nicotine metabolism
CYP2A6, CYP2B6, monooxygenases
Nicotine binding sites
An acetylcholine receptor agonist, binds tightly. notably to alpha 4 beta 2 which is located on GABA interneurons which is quickly desensitized disinhibiting dopamine release. alpha 7 controls Glu release
Nicotine tolerance
vomiting and dizziness go away quick but no tolerance to heart or vessel effects. Sensitization due to higher expression on alpha 4 beta 2 (most in PFC)
Bupropion
nAChR antagonist as a Treatment for nicotine withdrawal has higher affinity. also inhibits NAT and NET to act as antidepressant
Varenicline
partial nAChR agonist to reduce craving
Hypnotics
cause sleep and drowsiness (Zopiclone, Zolpidem)
Z-Drugs
orexin antagonists, melatonin agonists, anti histamines
Sedatives
anxiolytic, sedation, anesthesia, anti convulsant
Sedative charaterization
based on duration of length. short is used for preanesthetic or insomnia. long acting for anticonvulsants, muscle relaxants and anxiolytics
Sedative metabolism
CYP450 creates active metabolites
-chordiazepoxide, diazepam, midazolam
Benzodiazepines
sedative, Binds GABA between alpha and gamma to increase frequency of opening when GABA is present. Rapid tolerance