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52 Cards in this Set
- Front
- Back
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What neurotransmitters comprise the monoamines?
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DA
NE 5-HT |
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What neurotransmitters comprise the catecholamines?
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DA
NE Epi |
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What are the main cell bodies of dopamine?
Rate-limiting step of activation? Method of termination? |
SN-->striatum--caudate and putamen
Ventral tegmental area-->striatum Hypothalamic-pituitary Olfactory Retina RLS Activation: Tyrosine hydroxylase PResynaptic reuptake; monoamine oxidase, COMT |
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What is the most common dopamine receptor? Action? Location?
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D1; stimulation of adenylate cyclase, increased cAMP
Found in striatum, cortex, limbic system |
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Role of D2 receptor? Location?
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Inhibits adenylate cyclase; located in striatum
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Actions of neuroleptics?
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Calm nervous system based on blocking D2 receptors
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Haloperidol: mechanism, drug category
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D2 blocker, typical antipsychotic
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Clozapine: mechanism, drug category
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weak antagonism at D1 and D2, blocks 5HT2 receptors; atypical antipsychoic
(favorable balance in terms of side effects + drug benefits) |
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Mechanism of cocaine. Clinical significance?
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Blocks reuptake of DA, provides sensation of euphoria.
Too much DA can produce confusion, psychosis. Too little produces PD. Chronic cocaine use depletes DA stores, during withdrawal patient can become depressed bc receptors are denervated |
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MAO-B inhibitors: Mechanism
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block DA breakdown
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Amphetamines: mechanism
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promote presynaptic release of DA
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What are the main cell bodies of norepinephrine?
Rate-limiting step of activation? Method of termination? |
NE Cell bodies: locus ceruleus
RLS: Tyrosine hydroxylase (tyrosine-->DOPA) Termination: reuptake, COMT, MAO |
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Metabolites of dopamine?
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DOPAC, HVA
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Metabolites of norepinephrine?
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VMA (CNS), MHPG (Periphery)
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Receptors of norepinephrine?
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a1, a2, b1, b2
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Phenoxybenzamine: mechanism
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A1 blockers (for HTN)
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Phentolamine: mechanism
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A1 blocker; used for HTN
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Clonidine: mechanism
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A2 presynaptic autoreceptor agonist (decreases sympathetic tone; helpful for HTN)
Note: A2, B2 are presynaptic receptors; A1, B1 are postsynaptic receptors |
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Yohimbine
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a2 presynaptic antagonist , increases symp tone (increased arousal, panic, anxiety)
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What are B receptors thought to do?
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Activate cAMP in response to NE
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What are the main cell bodies of serotonin?
Rate-limiting step of activation? Method of termination? |
Serotonin cell bodies: doral raphe nuclei around cerebral aqueduct, caudal raphe nuclei in pons/medulla (project to SC)
RLS: availability of tryptophan Reuptake is primary method of inactivation; MAO 5-HIAA |
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Reserpine: mechanism
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depletes vesicular stores of 5-HT
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Fenfluramine: mechanism
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increases release of 5-HT
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Fluoxetine: mechanism
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Inhibit reuptake of 5-HT
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Amitriptyline: mechanism
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inhibits reuptake of 5-HT
(tricyclic antidepressant) |
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Serotonergic receptors?
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5-HT 1 (increases or decreases adenylate cyclex)
(receptors affect phosphatidylinositol systems) |
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What are the main cell bodies of acetylcholine?
Enzyme involves in synthesis? Method of termination? |
ACh primary cell bodies: forebrain nuclei of nucleus basalis of Mynert, septal nuclei
Connections to hippocampus, amygdala Synthetic enzyme: CAT Termination by both: Cholinesterase Reuptake |
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Roles of Ach?
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Memory, attn
REM Regulatin of bhvr Motor fn ANS |
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Botulinum toxin: mechanism
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inhibits Ach release
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Aricept: mechanism
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Achase inhibitor for AD
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Exelon: mechanism
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ACHase inhibitor for AD
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Reminyl: mechanism
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AChase inhibitor for AD
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Mestinon: mechanism
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Peripheral cholinesterase inhibitor for myasthenia gravis
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Cholinergic receptors
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Nicotinic at NMJ and ANS
Muscarinic in brain (some nicotinic there too) |
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Atropine: mechanism
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blocks muscarinic receptors: increases heart rate, slow GI motility
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Urecholine: mechanism
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aunotomic agonist
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Scopolamine: mechanism
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blocks mescarinic receptors, can cause memory loss
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Ditropan: mechanism
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autonomic antagonist, promotes retention of urine
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What are the main cell bodies of GABA?
Rate-limiting step of activation? Method of termination? |
GABA:
(maj inhibitory NT) Ubiquitously distributed; high [ ] in striatum, hthal, SC, colliculi, medial temp lobe Synthesized from glutamate Reuptake I suppose |
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GABA Receptors
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GABA A-chloride channel
GABA B receptors |
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Benzodiazepines: mechanism
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potentiate GABA by binding to receptor; used to tx anx, seizures, muscle spasms
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Vigabatrin: mechanism
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GABA transaminase inhibitor to tx epilepsy in Europe
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Topiramate: mechanism
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modulates GABA; Topamax
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Divalproex: mechanism
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modulates GABA; Depakote
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Gabapentin: mechanism
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modulates GABA; Neurontin
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Riduzole: mechanism
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decrease glutamatergic transmission (for ALS and epilepsy)
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Lamotrigine: mechanism
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decrease glutamatergic transmission; ALS and epilepsy tx
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Glutamate receptors
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NMDA (some use 2nd messengers)
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Why does cocaine cause chorea?
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increase in endogenous dopamine
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Stimulation of which dopamine receptor increases adenyl cyclase activity?
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D1
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Effect of clozapine on prolactin?
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No effect
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How is the activity of monoamines primarily terminated?
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Reuptake into presynaptic neuron
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