NBoA Exam 3 drugs

AM251

CB1 receptor inverse agonist

AM374

FAAH enzyme blocker - leads to elevated anandamide levels

AM404

anandamide transport inhibitor

AM630

CB2 receptor inverse agonist

CP55,940

high efficacy agonist at CB1 and CB2 receptors (more potent than THC)

GAT211

CB1 receptor positive allosteric modulator

HU-210

CB1 receptor agonist (very potent)

Nabilone/THC

Partial CB1 agonist

Spice/K2

Synthetic high efficacy CB1 receptor agonist

SR141716A (Rimonabant)

inverse CB1 agonist (used to treat obesity in Europe but withdrawn because of depressive psychiatric side effects

WIN55,212-2

CB1 receptor high efficacy agonist

oxymorphone

MOR agonist

naltrindole

DOR antagonist

enkephalins

endogenous *DOR and MOR opioid

synthesized from proenkephalin

analgesic, antidepressant, anxiolytic

endorphins

endogenous *MOR and DOR opioid

synthesized from proopiomelanocortin (POMC)

met-Enkephalin + more

analgesic + rewarding

dynorphins

endogenous KOR opioid

synthesized from prodynorphin

leu-Enkephalin + more

mixed effects on pain, aversive

endomorphins

endogenous MOR opioid

analgesic

naloxone

MOR, DOR, KOR antagonist

morphine

less potent opioid

significant B-arrestin induced tolerance

methynaloxonium

charged naloxone

doesn’t leave brain region

heroin

potent opioid

diacetyl morphine

fentanyl

HIGHLY potent opioid

favors g-protein independent processes

SR-17018

opioid

favors g-protein dependent process leading to minimal respiratory depression

TRV130

opioid

much lower B-arrestin activation minimizing tolerance

still abuse liability

BMS-986122

positive allosteric modulator of MOR

does not enhance down-regulation → less tolerance

methadone

longer active opioid with lesser withdrawal

used to ween heroin users off

hydromorphone

potent opioid agonist

buprenorphine

partial opioid agonist

butorphanol

partial opioid agonist

nalbuphine

opioid agonist (KOR) -antagonist (MOR)

naltrexone

opioid receptor antagonist

cotinine

metabolite of nicotine

used to monitor smoking habits as it remains in blood and hair

6-OH DA

lesions dopamine neurons

mecamylamine

nAChR antagonist

isoproterenol

direct sympathomimetic

phenylephrine

direct sympathomimetic

reboxetine

indirect sympathomimetic

norepinephrine reuptake inibitor

buproprion

indirect sympathomimetic

norepinephrine dopamine reuptake inibitor

scopolamine

nonsympathomimetic

strychnine

nonsympathomimetic

caffiene

nonsympathomimetic

cocaine

indirect sympathomimetic

DAT, NET, SERT

methamphetamine

indirect sympathomimetic

DAT, NET, SERT

amphetamine

indirect sympathomimetic

DAT, NET, SERT

methylphenidate

indirect sympathomimetic

DAT, NET

Ritalin

phenethylamine (PEA)

naturally occurring VMAT2 inhibitor

high first pass effect by monoamine oxidases

benzedrine

l-amph and d-amph

dexedrine

d-amph

methedrine

methamphetamine HCl

ephedrine

used to maintain BP during spinal anesthesia

amphetamine like

pargyline

enhances the lesioning effects of 6-OHDA

MAO-B inhibitor

desmethylimipramine

NE reupiake inhibitor

used to spare NE neurons from 6-OHDA lesions