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
|
(9!popup(ch34ref9))
(9!popup(ch34ref9))
(9!popup(ch34ref9))
|
|
|
|
|
|
|
|
|
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.
|