-
benztropine
- anticholinergic
- smooths ACh/DA activity in the basal ganglia
- inhibit DA transporter?
- NMDA antagonist?
-
trihexyphenidyl
- anticholinergic
- smooths ACh/DA activity in the basal ganglia
- inhibit DA transporter?
- NMDA antagonist?
-
dopamine
DA1R and DA2R agonist at nigrostriatal
-
LDopa
DA analogue at DA1/2R
-
carbidopa
peripheral ALAA decarboxylase I
-
benserazide
peripheral ALAA decarboxylase I
-
amantadine
- increase DA
- inhibit DA reuptake
- NMDA antagonist
-
bromocriptine
- D2 agonist (++)
- 5HT and alpha agonist
- ergot
-
lisuride
- D2 (+++)>D1 (+) agonist
- 5HT and alpha agonist
- ergot
-
pergolide
- D2 (+) agonist
- 5HT, alpha, and beta agonist
- ergot
-
cabergoline
- D2 (+++)> D1 (+/0) agonist
- 5HT and alpha agonist
- ergot
-
apomorphine
D2 (+++)> D1 (+) agoinst
-
pramipexole
D2 agonist (+++)
-
ropinirole
D2 (+++) agonist
-
entacapone
peripheral COMT I
-
-
selegiline
- selective, irrevesible MAO-B I
- inhibit tyramine reuptake
- inhibit NE release
- reduce oxidative damage (DA radicals)
- inhibit MPTP-->MPP+
(1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine)-->(1-methyl-4-phenylpyridinium)
-
rasagiline
highly selective irreversible MAO-B I
-
-
-
IFN-B1a
- (glycosylated)
- inhibition of peripheral Th1 cytokine
- BBB: decrease T cell MMPs and endothelial VCAM-1= decrease CNS infiltration
- (Matrix metalloproteinase)
- (vascular cell adhesion molecule 1)
-
IFN-B1b
- inhibition of peripheral Th1 cytokine
- BBB: decrease T cell MMPs and endothelial VCAM-1= decrease CNS infiltration
- (Matrix metalloproteinase)
- (vascular cell adhesion molecule 1)
-
glutiramer acetate
- PNS: promotes Th1-->Th2 shift
- BBB: no effect on MMPs/VCAM-1
- CNS: bystander suppresion by Th2
-
natalizumab
inhibit alpha-2 integrin= decrease lymphocyte/monocyte adhesion= decrease infiltration
-
opioids
- mu agonist
- kappa/sigma activation= decrease GABA= increase DA (disinhibition of DA N)
-
clonidine
- alpha-2 agonist
- reduces firing of NE N (inhibited by opioids)
-
meperidine
- mu agonist
- 5HT reuptake inhibitor
-
tramadol
- weak mu agonist
- blocks 5HT/NE reuptake
-
cocaine
- block DA reuptake
- anesthetic at high doses
-
amphetamines
- cause DA release by reverse vesicular transporter
- block DA/NE reuptake
- block MAO
-
methcathinone
analogue of methamphetamine and and cathinone
-
delta-9-tetrahydrocannabinol
- presynaptic CB1 agonist= inhibit Na+/Ca+ influx and K+ efflux
- disinhibition of DA neurons
-
lysergic and diethylamide
5HT R partial agonist
-
mescaline
5HT R partial agonist
-
psilocybin
5HT R partial agonist
-
nicotine
- decrease DA release in the nucleus accumbens
- decrease Glu= increase DA= euphoria
- GABA spikes before falling
- DA N excitation and disinhibition?
-
alcohol
- increase nicotinic/5HT3/GABA activity
- increase DA release
- block NMDA/kainate
- inhibit Ca+2 channels
- stimulates Gs
- change in lipid composition
- DA N excitation and disinhibition?
-
BDZ
- bind GABAa-gamma subunit= increase Cl- conductance= removal of inhibitory tone= increase Glu-mediated
- DA N disinhibition
-
-
pentathiol
short-acting BARB
-
nembutal
intermediate-acting BARB
-
seconal
intermediate-acting BARB
-
tuinal
intermediate-acting BARB
-
phenobarbital
long-acting BARB
-
gamma-hydroxy butyrate (GHB)
- activation of pre-/post-synaptic GABAb R
- GHB R binding
-
donepezil
selective non-competitive AChEI
-
rivastigmine
non-competitive AChEI and butyrylAChE I
-
-
galantamine
- enhance nicotine-mediated nicotinic activity by binding all alpha subunits
- weak competitive AChEI and butyrylAChE I
-
memantine
- non-competitive NMDA antagonist
- non-competitive nicotinic R antagonist at alpha7/8/9 subunits
- facilitates Glu synaptic release from hippocampal and cortical neurons
- non-competitive 5HT3 R blockate
-
-
-
-
-
clioquinol
beta-amyloid aggregation inhibitor
-
alzhemed
beta-amyloid aggregation inhibitor
-
cevimeline
M1/3 selective agonist
-
-
gingko biloba
- increase cerebral blood flow
- beta-amyloid aggregation inhibitor in-vivo at high concentration
- flavonoids (6%)= antioxidants
-
FGA
- D2 antagonist
- H1/alpha-1/M1 antagonist
-
chlorpromazine
low-potency FGA
-
-
haloperidol
high-potency FGA
-
pimozide
high-potency FGA
-
perphenazine
high-potency FGA
-
-
-
-
SGA
- D2 antagonist
- H1/alpha-1/M1 antagonist
- 5HT2A antagonist
-
aripiprazole
D2*>D3>5HT1A*>5HT2A>5HT2C>D4>alpha-1>H1>D1>M1
-
asenapine
5HT2C>5HT2A>D3>H1>D4>alpha-1>D2>D1>M1
-
clozapine
H1>M1>alpha-1>5HT2A>5HT2C>D4>D1>D2>D3>5HT1A*
-
lurasidone
5HT2A>D2>5HT1A>alpha-1>D1>5HT2C>H1>M1
-
olanzapine
H1>5HT2A>M1>5HT2C>D2>D4>D1>D3>alpha-1>5HT1A
-
paliperidone
5HT2A>D2>H1>D3>alpha-1>D1>5HT2C>D4>5HT1A>M1
-
quetiapine
H1>alpha-1>5HT2A>D2>5HT1A*>D1>D3>M1>D4>5HT2C
-
risperidone
5HT2A>alpha-1>D2>D4>D3>5HT2C>H1>5HT1A>D1>M1
-
ziprasidone
5HT2A>5HT2C>5HT1A*>D2>D3>alpha-1>D4>H1>D1>M1
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