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Ganong's Review of Medical Physiology, 26e > 
Neurotransmitters & Neuromodulators
Kim E. Barrett, Susan M. Barman, Heddwen L. Brooks, Jason X.-J. Yuan

TABLE 7–2
Pharmacology of a selection of receptors for some small-molecule neurotransmitters.

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
Net
Second
Neurotransmitter Receptor Channel Agonists Antagonists
Messenger 
E ects
+ + 
Glutamate AMPA   ↑Na , K AMPA CNQX, DNQX
+ +
Kainate   ↑Na , K Kainate CNQX, DNQX
+ +
NMDA   ↑Na , K , NMDA AP5, AP7
2+
Ca
+ 2+
mGluR1 ↑cAMP, ↓K , ↑Ca DHPG  
IP3, DAG
+ 2+
mGluR5 ↑IP3, DAG ↓K , ↑Ca Quisqualate  
+ 2+
mGluR2, ↓cAMP ↑K , ↓Ca DCG-IV  
mGluR3
2+
mGluR4, ↓cAMP ↓Ca L-AP4  
mGluR6-7
–
GABA GABAA   ↑Cl Muscimol Bicuculline, Gabazine,
Picrotoxin
+ 2+
GABAB ↑IP3, DAG ↑K , ↓Ca Baclofen Saclofen
–
Glycine Glycine   ↑Cl Taurine, β-alanine Strychnine
+ +
Acetylcholine NM   ↑Na , K Nicotine Tubocurarine,
Gallamine triethiodide
+ +
NN   ↑Na , K Nicotine, lobeline Trimethaphan
2+
M1, M3, M5 ↑IP3, DAG ↑Ca Muscarine, Bethanechol, Atropine, Pirenzipine
Oxotremorine (M1) (M1)
+
M2, M4 ↓cAMP ↑K Muscarine, Bethanechol Atropine, Tropicamide
(M2) (M4)
+
Norepinephrine α1 ↑IP3, DAG ↓K Phenylephrine Prazosin, Tamsulosin
+ 2+
α2 ↓cAMP ↑K , ↓Ca Clonidine Yohimbine
+
β1 ↑cAMP ↓K Isoproterenol, Atenolol, Esmolol
Dobutamine

β2 ↑cAMP   Albuterol Butoxamine

+
Serotonin 5HT1A ↓cAMP ↑K 8-OH-DPAT Metergoline,
Spiperone

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Net 
Second
Neurotransmitter Receptor Channel Agonists Antagonists
Messenger
E ects 
5HT1B ↓cAMP   Sumatriptan   
+
5HT1D ↓cAMP ↓K Sumatriptan  
+
5HT2A ↑IP3, DAG ↓K Dobutamine Ketanserin

5HT2C ↑IP3, DAG   α-Methyl-5-HT  

+
5HT3   ↑Na α-Methyl-5-HT Ondansetron
+
5HT4 ↑cAMP ↓K 5-Methoxytryptamine  

8-OH-DPAT, 8-hydroxy-N, N-dipropyl-2-aminotetralin; AMPA, α-amino-3-hydroxy-5-methyl-4-isoxazole-propionate;

DAG, diacylglycerol; DCG-IV, 2-(2, 3-dicarboxycyclopropyl)glycine; DHPG, 3-5 dihydroxyphenylglycine; IP3, inositol
triphosphate; L-AP4, 2-amino-4-phosphonobutyrate; NMDA, N-methyl-D-aspartate.

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