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 제품안내  신경약학   Pharmacology

Adrenergic Receptor

Adrenergic Receptor agonist & antagonist를 소개합니다.

TOCRIS
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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)
    *partial agonist
    †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.