TABLE 2. a2-Adrenergic Agents

Drug Name

Structure

Ki (nM) at human a2-AR subtypes

Reference

Agonists:

     

Epinephrine

A:1671

B:1851

C:318

(53)

(53)

(53)

Norepinephrine

A: 3677

B:1265
C:606

(53)

(53)

(53)

Clonidine

A:16.4 ± 1.4

C:10.2 ± 3.7

(33)

(33)

Apraclonidine

(p-amino-clonidine)

A: 31
B: 120
C: 97

(53)

(53)

(53)

UK 14304

A: 72

C: 210

(68)

(68)

Oxymetazoline

A: 3.3 ± 0.03
B: 754 ± 23
C: 31 ± 1

(53)

(53)

(53)

Dexmedetomidine

A: 8.08 ± 0.28

B: 5.91 ± 1.54

(38a)

(38a)

Guanabenz

A: 14

C: 59

(68)

(68)

Rauwolscine

(* indicates diastereomeric carbon--see Yohimbine)

A: 0.32 ± 0.02
B: 0.37 ± 0.05
C: 0.13 ± 0.01

(9)

(9)

(9))

Yohimbine

(* indicates diastereomeric carbon--see Rauwolscine)

A: 0.50 ± 0.02
B: 1.18 ± 0.06
C: 0.30 ± 0.02

(9)

(9)

(9)

RX 821002

{

A:0.8 ± 0.2
B:1.6 ± 0.4

(28)

(28)

WB 4101

A: 0.91 ± 0.03
B:4.34 ± 0.32
C:0.40 ± 0.04

(9)

(9)

(9)

ARC 239

A: 131 ± 16
B: 2.67 ± 0.01
C: 3.82 ± 0.45

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Phentolamine

A: 4.1 ± 0.3
B: 6.8 ± 0.9
C: 12.7 ± 0.6

(9)

(9)

(9)

BRL 44408

A: 5.35 ± 2.85

C: 227 ± 78

(33)

(33)

BAM 1303

A: 0.39 ± 0.03
B: 5.28 ± 0.66
C: 0.39 ± 0.05

(9)

(9)

(9)

Spiroxatrine

A: 5.5 ± 0.8
B: 0.19 ± 0.02
C: 0.13 ± 0.01

(9)

(9)

(9)

Idazoxan

A: 21 ± 3.4
B: 43 ± 5.5
C: 35 ± 9.7

(56a)

(56a))

(56a)

Prazosin

A: 302 ± 18
B: 30.6 ± 3.2
C: 10.7 ± 0.4

(9)

(9)

(9)

Mianserin

A: 7.0 ± 0.1
B: 27 ± 6

(11a)

(83)

A = a2a- AR subtype; B = a2b- AR subtype; C = a2c- AR subtype. Ki values at human receptors are expressed as mean +/- S.E.M. when available.

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published 2000