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NPP Final - Flashcards

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Class:BIO 3623 - Neuropsychopharmacology
Subject:Biology
University:University of Texas - San Antonio
Term:Fall 2011
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Apomorphine
Apomorphine is a non-selective dopamine agonist which activates both D1-like and D2-like receptors
SKF 38393  a selective D1/D5 receptor partial agonist.
Quinpirole selective D2 and D3 receptor agonist.
SCH 23390  D1 receptor antagonist
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Haloperidol Blocks D2 Receptors
a1 receptor Gq
increase in Pi, increase Ca2+


phenylephrine Phenylephrine is a selective a1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure.
Prazosin a1 adrenergic receptor antagonist
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Clonidine a2 adrenergic receptor agonist
Yohimbine a2 adrenergic receptor antagonist
albuterol B adrenergic receptor agonist
propanolol B adrenergic receptor antagonist
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vesamicol acting presynaptically by inhibiting acetylcholine uptake and reducing its release.
Black widow spider venom stimulates ACh release (agonist)
Botulinum toxin Inhibits Ach release (antagonist)
Hemicholinium - 3 blocks the reuptake of choline causing an acetylcholine depletion.
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sarin inhibits acetylcholinesterase
Nicotine stimulates nicotinic receptors
Curare Blocks nicotinic receptors
Muscarine stimulates muscarinic receptors
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atropine blocks muscarinic receptors
phenelzine Phenelzine is a non-selective and irreversible monoamine oxidase inhibitor (MAOI) which is used as an antidepressant
increases ACh levels.
AMPT Alpha-methyl-p-tyrosine is a tyrosine hydroxylase enzyme inhibitor.
Depletes catecholamine
Reserpine Depletes catecholamines by inhibiting vesicular uptake.
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6-hydroxy-dopamine damages/destroys catecholinergic neurons
amphetamine Releases catecholamines
Cocaine inhibits catecholamine reuptake
Ionotropic receptors "nicotinic receptors"
classic "non selective" cation channel.
mediate EPSPs
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Metabotropic Receptors "muscarinic" receptors
tyrosine hydroxylase tyrosine --> DOPA
RATE LIMITING STEP!!
Aromatic L- Amino acid decarboxylase DOPA---> Dopamine
Dopamine B-hydroxylase Dopamine --> NE
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phenylpropargylamine inhibits Dopamine B Hydroxylase so that Dopamine does not become NE
Dopamine Receptors D1 & D5 Gs
increases cAMP production = increase dopamine synthesis
Dopamine Receptors D2, D3 & D5 Gi
decreases cAMP production = increase dopamine synthesis

Dopamine catabolizes into ____ HVA
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mesocorticolimbic Dopamine System Ventral Tegmental Area --> cortex and limbic system
Nigrostriatal Dopamine System Substantia nigra --> striatum
tryptophan hydroxylase Tryptophan hydroxylase is an enzyme () involved in the synthesis of the neurotransmitter serotonin.

Tryptophan --> 5-HTP
aromatic L amino acid decarboxylase 5-HTP --> serotonin (5-HT)
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PCPA inhibits tryptophan hydroxylase.
antagonist
PCA releases serotonin
5-HT 1 receptors -inhibit serotonin release
-agonist : buspirone
-antagonist: WAY 100
5-HT 2 Receptor metabotropic
Gq, PLC and Pi turnover
agonist : LSD
antagonist: ketanserin
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5-HT 3 receptors ionotropic
acts as classic NT "fast" EPSPs
5-HT 4 receptors metabotropic
Gs; increase cAMP, PKA
agonists reduce IBS
5- HT metabolizes into _____ 5 - HIAA
para - chlorophenylalanine  irreversible inhibitor of tryptophan hydroxylase, which is a rate-limiting enzyme in the biosynthesis of serotonin.
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reserpine depletes 5-HT by inhibiting vesicular uptake
glutaminase glutamate --> glutamine
presynaptic terminal
glutamine synthase glutamate --> glutamine
occurs in the astrocyte
AMPA ligand gated cationic channel.
conduct NA+ into cell

agonist: AMPA
antag: CNQX
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Kainate ligand gated cationic channel
conduct NA2 + into cell

agonist: Domoic Acid
antag: CNQX
NMDA receptor The NMDA receptor, a glutamate receptor, is the predominant molecular device for controlling synaptic plasticity and memory function.

ligand and voltage gated
removes Mg 2+ and allows influx of Na + ions

Agonist: NMDA
Antagonist: AP-5, PCP, ketamine
Benzodiazapines anti anxiety drugs

should not be taken with alcohol because they act on the same receptors
Muscimol GABAa Agonist
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Biciculine GABAa antagonist
picroloxin GABAa noncompetitive antagonist
Baclofen GABAb agoninst
Phaclofen GABAb antagonist
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GABAb Receptor metabotropic
Gi: inhibits AC, decreases cAMP
Go: increase PLA2, K+ conductance and calcium influx
Glycine inhibitory like GABA
"obligate agonist" for NMDA receptors
antagonist: strychmine
Histamine excitatory
derived from histamine
H1 receptors Primarily Gq, PLC, increase Pi turnover.
                 Gs, increase cAMP

involved in inflammation
antagonist: Claritin
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H2 receptors Gs, increase cAMP, decrease AA
mediate HCl release from stoman
antagonist: Zantac
Adenosine primarily inhibitory via presynaptic effects
involved in sleep and arousal

Peptide NT distinct synthesis mechanism - synthesized in soma
frequency dependent release- typically requires repetitive presynaptic activity
Opioid Peptides ekaphalins
endorphins
dynorphins (opioids)
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Opiates alkaloids
not produced in the brain
activate opioid receptors

addictive opiates on mu receptors, these are coupled to Gi
Anandomide produced naturally by the brain and has the same effect as THC

good use for forgetting
inverse agonist In the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.
indolamine derived hallucinogens psilocybin, LSD, DMT

Serotonin derived
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phenylethylamine derived hallucinogens mescaline, MDA, MDMA

Dopamine system
Dissociative anesthetics PCP, Ketamine, MK-801
Type 1 Bipolar disorder Type 2 Bipolar disorder Severe mood swings



milder mood swings
Pure Food and Drug Act 1906
Regulated labeling of patent medication

created the FDA
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Harrison Act 1914
Regulated the dispensing and use of opioid drugs and Cocain
18th consitutional amendment 1920
banned alcohol sales except for medicinal use (prohibition)
Marijuana Tax Act 1937
Banned non medicinal use of cannabis
Controlled Substance Act 1970
established the scheduling of controlled substances and created the DEA
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Scheduling of controlled Substances I: highly abused. No medicinal purpose                                                                    (LSD, heroin, mescaline, MDMA)
II: highly abused. Highly addictive
              (opium, cocaine, PCP)
III: less abused than I or II
               (barbituates. some narcotics)
IV: less abuse potential than III
                (valium, xanax)
V: less abuse potential than IV
                 cough suppressents

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 Apomorphine
Apomorphine is a non-selective dopamine agonist which activates both D1-like and D2-like receptors
 SKF 38393 a selective D1/D5 receptor partial agonist.
 Quinpiroleselective D2 and D3 receptor agonist.
 SCH 23390 D1 receptor antagonist
 HaloperidolBlocks D2 Receptors
 a1 receptorGq
increase in Pi, increase Ca2+


 phenylephrinePhenylephrine is a selective a1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure.
 Prazosina1 adrenergic receptor antagonist
 Clonidinea2 adrenergic receptor agonist
 Yohimbinea2 adrenergic receptor antagonist
 albuterolB adrenergic receptor agonist
 propanololB adrenergic receptor antagonist
 vesamicolacting presynaptically by inhibiting acetylcholine uptake and reducing its release.
 Black widow spider venomstimulates ACh release (agonist)
 Botulinum toxinInhibits Ach release (antagonist)
 Hemicholinium - 3blocks the reuptake of choline causing an acetylcholine depletion.
 sarininhibits acetylcholinesterase
 Nicotinestimulates nicotinic receptors
 CurareBlocks nicotinic receptors
 Muscarinestimulates muscarinic receptors
 atropineblocks muscarinic receptors
 phenelzinePhenelzine is a non-selective and irreversible monoamine oxidase inhibitor (MAOI) which is used as an antidepressant
increases ACh levels.
 AMPTAlpha-methyl-p-tyrosine is a tyrosine hydroxylase enzyme inhibitor.
Depletes catecholamine
 ReserpineDepletes catecholamines by inhibiting vesicular uptake.
 6-hydroxy-dopaminedamages/destroys catecholinergic neurons
 amphetamineReleases catecholamines
 Cocaineinhibits catecholamine reuptake
 Ionotropic receptors"nicotinic receptors"
classic "non selective" cation channel.
mediate EPSPs
 Metabotropic Receptors"muscarinic" receptors
 tyrosine hydroxylasetyrosine --> DOPA
RATE LIMITING STEP!!
 Aromatic L- Amino acid decarboxylaseDOPA---> Dopamine
 Dopamine B-hydroxylaseDopamine --> NE
 phenylpropargylamineinhibits Dopamine B Hydroxylase so that Dopamine does not become NE
 Dopamine Receptors D1 & D5Gs
increases cAMP production = increase dopamine synthesis
 Dopamine Receptors D2, D3 & D5Gi
decreases cAMP production = increase dopamine synthesis

 Dopamine catabolizes into ____HVA
 mesocorticolimbic Dopamine SystemVentral Tegmental Area --> cortex and limbic system
 Nigrostriatal Dopamine SystemSubstantia nigra --> striatum
 tryptophan hydroxylaseTryptophan hydroxylase is an enzyme () involved in the synthesis of the neurotransmitter serotonin.

Tryptophan --> 5-HTP
 aromatic L amino acid decarboxylase5-HTP --> serotonin (5-HT)
 PCPAinhibits tryptophan hydroxylase.
antagonist
 PCAreleases serotonin
 5-HT 1 receptors-inhibit serotonin release
-agonist : buspirone
-antagonist: WAY 100
 5-HT 2 Receptormetabotropic
Gq, PLC and Pi turnover
agonist : LSD
antagonist: ketanserin
 5-HT 3 receptorsionotropic
acts as classic NT "fast" EPSPs
 5-HT 4 receptorsmetabotropic
Gs; increase cAMP, PKA
agonists reduce IBS
 5- HT metabolizes into _____5 - HIAA
 para - chlorophenylalanine irreversible inhibitor of tryptophan hydroxylase, which is a rate-limiting enzyme in the biosynthesis of serotonin.
 reserpinedepletes 5-HT by inhibiting vesicular uptake
 glutaminaseglutamate --> glutamine
presynaptic terminal
 glutamine synthaseglutamate --> glutamine
occurs in the astrocyte
 AMPAligand gated cationic channel.
conduct NA+ into cell

agonist: AMPA
antag: CNQX
 Kainateligand gated cationic channel
conduct NA2 + into cell

agonist: Domoic Acid
antag: CNQX
 NMDA receptorThe NMDA receptor, a glutamate receptor, is the predominant molecular device for controlling synaptic plasticity and memory function.

ligand and voltage gated
removes Mg 2+ and allows influx of Na + ions

Agonist: NMDA
Antagonist: AP-5, PCP, ketamine
 Benzodiazapinesanti anxiety drugs

should not be taken with alcohol because they act on the same receptors
 MuscimolGABAa Agonist
 BiciculineGABAa antagonist
 picroloxinGABAa noncompetitive antagonist
 BaclofenGABAb agoninst
 PhaclofenGABAb antagonist
 GABAb Receptormetabotropic
Gi: inhibits AC, decreases cAMP
Go: increase PLA2, K+ conductance and calcium influx
 Glycineinhibitory like GABA
"obligate agonist" for NMDA receptors
antagonist: strychmine
 Histamineexcitatory
derived from histamine
 H1 receptorsPrimarily Gq, PLC, increase Pi turnover.
                 Gs, increase cAMP

involved in inflammation
antagonist: Claritin
 H2 receptorsGs, increase cAMP, decrease AA
mediate HCl release from stoman
antagonist: Zantac
 Adenosineprimarily inhibitory via presynaptic effects
involved in sleep and arousal

 Peptide NTdistinct synthesis mechanism - synthesized in soma
frequency dependent release- typically requires repetitive presynaptic activity
 Opioid Peptidesekaphalins
endorphins
dynorphins (opioids)
 Opiatesalkaloids
not produced in the brain
activate opioid receptors

addictive opiates on mu receptors, these are coupled to Gi
 Anandomideproduced naturally by the brain and has the same effect as THC

good use for forgetting
 inverse agonistIn the field of pharmacology, an inverse agonist is an agent that binds to the same receptor as an agonist but induces a pharmacological response opposite to that agonist.
 indolamine derived hallucinogenspsilocybin, LSD, DMT

Serotonin derived
 phenylethylamine derived hallucinogensmescaline, MDA, MDMA

Dopamine system
 Dissociative anestheticsPCP, Ketamine, MK-801
 Type 1 Bipolar disorder Type 2 Bipolar disorderSevere mood swings



milder mood swings
 Pure Food and Drug Act1906
Regulated labeling of patent medication

created the FDA
 Harrison Act1914
Regulated the dispensing and use of opioid drugs and Cocain
 18th consitutional amendment1920
banned alcohol sales except for medicinal use (prohibition)
 Marijuana Tax Act1937
Banned non medicinal use of cannabis
 Controlled Substance Act1970
established the scheduling of controlled substances and created the DEA
 Scheduling of controlled SubstancesI: highly abused. No medicinal purpose                                                                    (LSD, heroin, mescaline, MDMA)
II: highly abused. Highly addictive
              (opium, cocaine, PCP)
III: less abused than I or II
               (barbituates. some narcotics)
IV: less abuse potential than III
                (valium, xanax)
V: less abuse potential than IV
                 cough suppressents

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