Adrenoceptor-selective Ligands

α-Adrenoceptor Selective

β-Adrenoceptor Selective

 Adrenergic Uptake Inhibitors

→ α1-Adrenoceptor Selective
→ α2-Adrenoceptor Selective
→ General α-Adrenoceptors

→ β1-Adrenoceptor
→ β2-Adrenoceptor
→ β3-Adrenoceptor
→ General β-Adrenoceptors

 

The following tables summarise the properties of these receptors and include selected examples of adrenoceptor-selective ligands.

α1-Adrenoceptor Pharmacology
Receptor Subtype α1A α1B α1D
Transduction
Mechanism		 Activates Gp/q, PI turnover, [Ca2+]i.c., activates voltage-gated
Ca2+ channels
Selective Agonists A 61603 (1052)
Oxymetazoline (1142)		 unknown unknown
Non-subtype
Selective Agonists		 Cirazoline (0888)
M-6434 (0461)		 Cirazoline (0888)
M-6434 (0461)		 Cirazoline (0888)
M-6434 (0461)
Selective Antagonists RS 17053 (0985)
RS 100329 (1325)
WB 4104 (0946)		 –
–		 BMY 7378 (1006)
Non-subtype Selective
Antagonists		 Corynanthine (1143)
Prazosin (0623)		 corynanthine (1143)
Prazosin (0623)		 Corynanthine (1143)
Prazosin (0623)
 
α2-Adrenoceptor Pharmacology
Receptor Subtype α2A α2B α2C
Transduction
Mechanism		 Activates Gi/o, ↓cAMP, inhibits voltage-gated Ca2+ channels, activates Ca2+ dependent K+ channels
Selective Agonists Oxymetazoline* (1142)
Guanfacine (1030)		 unknown unknown
Selective Antagonists BRL 44408 (1133) ARC 239 (0928)
Imiloxan (0986)
Prazosin (0623)		 Rauwolscine† (0891)
Non-subtype
Selective Agonists		 Clonidine (0690)
UK 14,304 (0425)		 Clonidine (0690)
UK 14,304 (0425)		 Clonidine (0690)
UK 14,304 (0425)
Non-subtype Selective
Antagonists		 RS 79948 (0987)
Yohimbine (1127)
Rauwolscine (0891)
Efaroxan (0792)
Idazoxan (0793)		 RS 79948 (0987)
Yohimbine (1127)
Rauwolscine (0891)
Efaroxan (0792)
Idazoxan (0793)		 RS 79948 (0987)
Yohimbine (1127)
Rauwolscine (0891)
Efaroxan (0792)
Idazoxan (0793)
* partial agonist    † 10-20 fold selective for α2C
β-Adrenoceptor Pharmacology
Receptor Type β1 β2 β3 β4
Transduction
Mechanism		 Adenylyl cyclase
(via Gs)		 Adenylyl cyclase
(via Gs) or /↓ adenylyl
cyclase		 Adenylyl cyclase
↓Adenylyl cyclase		 cAMP levels,
stimulation of
cAMP-dependent
protein kinase
(via Gs)
Selective
Agonists		 Xamoterol* (0950) Procaterol (1102)
Salbutamol (0634)		 BRL 37344 (0948)
CGP 12177* (1134)
ZD 7114 (0930)		 Unknown
Selective
Antagonists		 Betaxolol (0906)
Bisoprolol (0914)
(±)-Atenolol (0387)
Practolol (0831)		 ICI 118551 (0821)
[3H]-ICI 118551 (R821)		 – Unknown
* partial agonist
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