TABLE 1. a1-Adrenergic Receptor subtypes: nomenclature, proximal effects, receptor pharmacology and distribution in the CNS

Present nomenclature

Pharmacologically identified as:

Cloned as:

G protein

Second Messenger

Subtype-selection Agonists

Subtype-selective Antagonists

Human MrNA

Human protein

a1A

a1A

a1c

Gq

G11

G14

Ca2+

PLC

PLA2

PLD

oxymetazoline

5-methyluradipil

(+)-niguldipine

A-61603

SNAP-5089

KMD-3213

RS 17053

WB4101

Cerebellum

cerebral cortex

pituitary

Cerebral cortex

(frontal, temporal, parietal lobe)

a1B

a1B

a1b

Gq

G11

G14

G16

Gh

Same as above

AH11110A

spiperone

Cerebellum

cerebral cortex

Cerebral cortex

(frontal, temporal, parietal lobe)

a1D

Not discovered

a1a

a1d a1a/d

Gq

G11

Same as above

BMY 7378

SKF 105854

(+)-discretamine

Cerebellum cerebral cortex

Not determined

* Subtype selective agents are listed, but relative orders of potency and Ki values are not given, as they are in Table II for a2AR agents and III for bAR agents, because these values for a1AR subtypes often vary between tissues and for cloned versus native receptors, particularly for (+)- niguldipine and 5- methyluradipil.
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published 2000