Pharmacology
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All Products
New Products
Small Molecules
Peptides
Controlled Substances
Toxins
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Screening Libraries
Ligand Sets
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Research Area
Cancer
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α1-Adrenergic Receptor Data
| Receptor Subtype | α1A | α1B | α1D |
|---|
| Transduction Mechanism | Activates Gp/q, ↑ PI turnover, ↑[Ca2+]i.c.) and activates voltage-gated Ca2+ channels | ||
| Localization | CNS, heart, liver, prostate, urethra | CNS, somatic arteries and veins, spleen, kidney | CNS, aorta, bladder, prostate |
| Tissue Function | Smooth muscle contraction, myocyte hypertrophy, activation of sarcolemmal Na+-H+ exchanger | Smooth muscle contraction, cardiac growth and contractile function | Smooth muscle contraction |
| Selective Agonists |
A 61603 (1052) Oxymetazoline (1142) |
Unknown | Unknown |
| Non-subtype Selective Agonists |
Cirazoline (0888) (R)-(-)-Phenylephrine hydrochloride (2838) |
Cirazoline (0888) (R)-(-)-Phenylephrine hydrochloride (2838) |
Cirazoline (0888) (R)-(-)-Phenylephrine hydrochloride (2838) |
| Selective Antagonists |
RS 17053 (0985) RS 100329 (1325) SNAP 5089 (2398) WB 4101 (0946) Tamsulosin (3050) |
Rec 15/2615 (3284) | BMY 7378 (1006) |
| Non-subtype Selective Antagonists |
Prazosin (0623) Doxazosin (2964) Alfuzosin (3305) |
Prazosin (0623) Doxazosin (2964) Alfuzosin (3305) |
Prazosin (0623) Doxazosin (2964) Alfuzosin (3305) |
α2-Adrenergic Receptor Data
| Receptor Subtype | α2A | α2B | α2C |
|---|
| Transduction Mechanism | Activates Gi/o, ↓ PI turnover, inhibits voltage-gated Ca2+ channels, activates voltage-gated Ca2+ dependent K+ channels | ||
| Localization | Brain, spleen, kidney, aorta, lung, skeletal muscle, heart, liver | Spleen, kidney, aorta, lung, skeletal muscle, heart, liver | Brain, kidney, aorta, lung, skeletal muscle, heart, spleen |
| Tissue Function | Hypotension, sedation, analgesia, hypothermia, anesthesia, inhibition of noradrenalin release | Vasoconstriction | Presynaptic inhibition of noradrenalin release |
| Selective Agonists |
Oxymetazoline* (1142) Guanfacine (1030) |
Unknown |
(R)-(+)-m-Nitrobiphenyline oxalate (2948) ST 91 (2638) |
| Non-subtype Selective Agonists |
Clonidine (0690) UK 14,304 tartrate (2466) |
Clonidine (0690) UK 14,304 tartrate (2466) |
Clonidine (0690) UK 14,304 tartrate (2466) |
| Selective Antagonists | BRL 44408 (1133) |
ARC (0928) Imiloxan (0986) Prazosin (0623) |
JP 1302 (2666) Rauwolscine† (0891) |
| Non-subtype Selective Antagonists |
RS 79948 (0987) Yohimbine (1127) Efaroxan (0792) Idazoxan (0793) |
RS 79948 (0987) Yohimbine (1127) Efaroxan (0792) Idazoxan (0793) |
RS 79948 (0987) Yohimbine (1127) Efaroxan (0792) Idazoxan (0793) |
†10-20 fold selective for α2C
β-Adrenergic Receptor Data
| Receptor Subtype | β1 | β2 | β3 |
|---|
| Transduction Mechanism | ↑ Adenylyl cyclase (via Gs) | ||
| Localization | CNS, heart, coronary artery, lung, spleen, kidney, liver, muscle | CNS, heart, lung, spleen, kidney, liver, skeletal muscle | Adipose tissue, gall bladder, small intestines, stomach, prostate, left atrium, bladder, vascular endothelium |
| Tissue Function | Tachycardia, coronary vasodilation, increase heart contractile force, apoptosis, relaxation of colon and esophagus | Hypotension, smooth muscle relaxation e.g. bronchodilation, inhibition of apoptosis | Lipolysis, glucose uptake, cardioinhibition, relaxation of colon, esophagus and bladder |
| Key Compounds | Ki values (nM) |
|---|
| Agonists |
BRL 37344 (0948) CGP 12177* (1134) Cimaterol (0435) Pindolol (0994) Salbutamol (0634) |
1750 0.9 - 3.4 - |
1120 4 - 2.3 - |
287 88 4700 11 53000 |
| Antagonists |
ICI 118,551 (0821) L-748,337 (2760) |
120 390 |
1.2 204 |
257 4 |
*β3 partial agonist, β1/β2
References
Bylund et al (1994) Pharmacol.Rev. 46 121.Hieble et al (1995) J.Med.Chem. 38 3415. Strosberg and Pietri-Rouxel (1996) TiPS 17 373. Docherty et al (1998) Eur.J.Pharmacol. 361 1. Robinson and Hudson (1998) Tocris Reviews. No. 8.