Question | Answer |
Reserpine | -inhibits VMAT -> depletes vesicular stores of monoamines (DA, NE, 5-HT)
-decreases hypertension
-15% of people taking reserpine for hypertension developed depressive-like symptoms
- Parkinsonian side effects |
L-DOPA | -Patients with Parkinson’s were
given L-DOPA (a version of the
dopamine precursor DOPA) to
enhance DA transmission
-Many patients obtained relief
from EPS, but some developed
an acute, positive-sx psychosis
as a treatment side effect. |
AMPT | -(α‐methyl‐p-tyrosine)competes for tyrosine
binding site; no clinical use
-blocks catecholamine synthesis by blocking Tyrosine Hydroxylase |
SKF 38393 | -D1R agonist: stimulates locomoter activity (i.e. grooming)
-no clinical use |
SCH23390 | -D1R antagonist
-no clinical use |
Haloperidol | -D2R antagonist: used to treat schizophrenia (classic antipsychotic)
-Treats POSITIVE symptoms of schizophrenia with little effect on negative or cognitive symptoms
-decreases reinforcing properties of cocaine but also impairs locomotion |
Amphetamine | -blocks DAT/NET, releases DA/NE b/c reversal of VMAT
-used to treat ADHD: Amphetamine + dextroamphetamine (Adderall™) |
Cocaine | ? |
Methylphenidate | -blocks DAT and to a lesser extent NET
-used to treat ADD= Ritalin
-Abuse liability of methylphenidate is not related to DAT occupancy or peak plasma levels of methylphenidate, but appears to be
related to the magnitude of the increase in DA/unit time |
Atomoxetine | -blocks NET, non stimulant
-increases DA/NE in FC, not striatum, b/c more DAT in striatum
-used to treat ADD |
Clonidine | -alpha2-adrenergic agonist that stimulates autoreceptors and inhibits noradrenergic cell firing.
-used to reduce hypertension and opiate withdrawal
-side effects: sedation, feelings of sleepiness |
Vesamicol | -drug that blocks the vesicular ACh transporter |
HC-3 (hemicholinium-3) | -drug that blocks the choline transporter in cholinergic nerve terminal (inhibits choline reuptake) |
Physostigmine | -blocks AChE activity
-Eserine
-symptoms include slurred speech, mental confusion, hallucinations, loss of reflexes, convulsions, coma, and death
-isolated from Calabar beans |
Muscarine | -alkaloid that stimulates muscarinic cholinergic receptors that are selectively stimulated by muscarine |
Scopolamine | -drug that blocks muscarinic receptors
-found in night shade and henbane
-causes cognitive impairments, delirium, and tachycardia (hallucinogen) |
p‐chlorophenylalanine (PCPA) | -drug that irreversibly inhibits tryptophan hydroxylase, blocking 5-HT synthesis |
p‐chloroamphetamine (PCA) | Drug similar in structure to amphetamine that stimulates 5-HT release. It is also neurotoxic at high doses |
8‐OH‐DPAT | agonist at 5-HT1A receptor
can cause: hyperphagia(autoreceptors), hypothermia, anxiolytic |
Buspirone | -agonist at 5-HT1A receptor
-symptoms include increased appetite,reduced axiety, reduced alcohol cravings, and a lower body temp.
-prescribed as an antianxiety medication |
WAY100635 | -drug that selectively inhibits 5-HT1A receptors |
Fluoxetine | (Prozac)
-selectively blocks the 5-HT transporter
-clinical use: antidepressant |
Ketanserin | -nonselective 5-HT2A receptor antagonists
-used to decrease hypertension |
allylglycine | -blocks GABA synthesis
-causes convulsions |
picrotoxin | -noncompetitive antagonist at GABA(A) receptor
-causes convulsions |
Benzodiazepine | -class of drugs that act as CNS depressants through positive allosteric modulation of GABA(A) receptor activity
-prescribed as anti-anxiety meds:
-high abuse liability
-intense side effects:sedative/hypnotic effects, muscle relaxant, anti-convulsant |
Diazepam and Chlordiazepoxide | -Benzodiazepines
-used clinically in detox to minimize alcohol withdrawal symptoms |
Barbiturate (class of drug) | -positive allosteric modulators;increase mean open time of GABA(A) channel
• Have similar effects as BDZs |
muscimol | -classic GABA(A) receptor agonist
-Causes macroscopia,hyperthermia, pupil dilation,increased mood, difficulties
concentrating, anorexia, ataxia, hallucinations |
bicuculline | -competitive antagonist at GABA(A) receptor
-causes seizures |
Baclofen (Lioresal) | -selective agonist for the GABA(B) receptor
-used as muscle relaxant and anti-spastic agent |
NBQX | -antagonist that blocks both AMPA and kainate receptors but has no effect on NMDA receptors |
phencyclidine (PCP) | -binds to the PCP site and acts as noncompetitive antagonist of the NMDA receptor
-dissociative anesthetic that was once used medicinally but now is only taken recreationally |
Ketamine | -drug that binds to PCP site and acts as noncompetitive antagonist at NMDA receptor
-dissociative anesthetic used in both human and veterinary medicine, and it is also used recreationally |