Dr.

Mrinal sanaye 2017

Transmitter Anatomy Receptor Receptor Mechanisms

Subtypes and Antagonists
Preferred
Agonists

Acetylcholine Cell bodies at all levels; Muscarinic (M1): Pirenzepine, Excitatory: in K+ conductance;
long and short muscarine atropine IP3, DAG
connections

Muscarinic (M2): Atropine, Inhibitory: K+ conductance;

muscarine, methoctramine cAMP
bethanechol

Motoneuron-Renshaw Nicotinic: Dihydro-- Excitatory: cation

cell synapse nicotine erythroidine, - conductance
bungarotoxin

Dopamine Cell bodies at all levels; D1 Phenothiazines Inhibitory (?): cAMP

short, medium, and
long connections

D2: Phenothiazines, Inhibitory (presynaptic): Ca2+;

bromocriptine butyrophenones Inhibitory (postsynaptic): in K+
conductance, cAMP

GABA Supraspinal and spinal GABAA: Bicuculline, Inhibitory: Cl–conductance

interneurons involved muscimol picrotoxin
in pre- and
postsynaptic inhibition

GABAB: baclofen 2-OH saclofen Inhibitory (presynaptic): Ca2+

conductance; Inhibitory
(postsynaptic): K+
conductance

Introduction to CNS
 Dr. Mrinal sanaye 2017

Transmitter Anatomy Receptor Subtypes Receptor Mechanisms

and Preferred Antagonists
Agonists

Glutamate Relay neurons at all N-Methyl-D- 2-Amino-5- Excitatory: cation

levels and some interneurons aspartate (NMDA): phosphonovalerate, conductance,
NMDA dizocilpine particularly Ca2+

AMPA: AMPA CNQX Excitatory: cation

conductance

Kainate: kainic acid,

domoic acid

Metabotropic: ACPD, MCPG Inhibitory

quisqualate (presynaptic): Ca2+
conductance
cAMP; Excitatory:
K+ conductance,
IP3, DAG

Glycine Spinal interneurons Taurine, -alanine Strychnine Inhibitory: Cl–

and some brain stem conductance
interneurons

5- Cell bodies in 5-HT1A: LSD Metergoline, Inhibitory: K+

Hydroxytryptamine midbrain and pons spiperone conductance,
(serotonin) project to all levels cAMP

5-HT2A: LSD Ketanserin Excitatory: K+

conductance, IP3,
DAG

5-HT3: 2-methyl-5-HT Ondansetron Excitatory: cation

conductance

5-HT4 Excitatory: K+
conductance
 Dr. Mrinal sanaye 2017

Transmitter Anatomy Receptor Subtypes Receptor Antagonists Mechanisms

and Preferred
Agonists

Norepinephrine Cell bodies in 1: phenylephrine Prazosin Excitatory: K+ conductance,

pons and brain IP3, DAG
stem project to
all levels

2: clonidine Yohimbine Inhibitory (presynaptic):

Ca2+ conductance;
Inhibitory: K+ conductance,
cAMP

1: isoproterenol, Atenolol, practolol Excitatory: K+ conductance,

dobutamine cAMP

2: albuterol Butoxamine Inhibitory: may involve in

electrogenic sodium pump;
cAMP

Histamine Cells in ventral H1: 2(m- Mepyramine Excitatory: K+ conductance,

posterior fluorophenyl)- IP3, DAG
hypothalamus histamine

H2: dimaprit Ranitidine Excitatory: K+ conductance,

cAMP

H3: R--methyl- Thioperamide Inhibitory autoreceptors

histamine

Transmitter Anatomy Receptor Subtypes Receptor Mechanisms

and Preferred Antagonists
Agonists
 Dr. Mrinal sanaye 2017

Opioid peptides Cell bodies at all Mu: bendorphin Naloxone Inhibitory (presynaptic):
levels; long and Ca2+ conductance, cAMP
short
connections

Delta: enkephalin Naloxone Inhibitory (postsynaptic): K+

conductance, cAMP

Kappa: dynorphin Naloxone

Tachykinins Primary sensory NK1: Substance P Aprepitant Excitatory: K+ conductance,

neurons, cell bodies methylester, IP3, DAG
at all levels; long and aprepitant
short connections

NK2

NK3

Endocannabinoi Widely CB1: Anandamide, Rimonabant Inhibitory (presynaptic):

ds distributed 2- Ca2+ conductance, cAMP
arachidonyglycerol