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 제품안내  신경약학   Pharmacology

Dopamine Receptor

Dopamine Receptor agonist & antagonist를 소개합니다.

TOCRIS
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    Dopamine Receptor Data
    Receptor Subtype D1-like Receptors D2-like Receptors
    D1 D5 D2 D3 D4
    G protein Gs Gs Gi/o Gi/o Gi/o
    Transduction Mechanism ↑ AC, ↑ PLC, ↑ L-type Ca2+ channels ↑ AC ↓ AC, ↑ [Ca2+]i, K+ conductance, ↓ Ca2+ conductance ↓ AC, activation of MAP kinase ↓ AC, ↓ Ca2+ conductance
    Localisation Caudate, putamen, nucleus accumbens, olfactory tubercle Hippocampus, hypothalamus Caudate, putamen, nucleus accumbens, olfactory tubercle Nucleus accumbens, olfactory tubercle, islands of Calleja Frontal cortex, midbrain, amygdala, cardiovascular system
    Likely Physiological Roles Locomotion, reward, reinforcement, learning and memory, renin secretion Learning and memory Locomotion, reward, reinforcement, learning and memory Locomotion, possible role in cognition and emotion Mostly unknown - possible role in cognition and emotion, hypertension

    Key Compounds Ki Values (nM)
    D1-like Agonists SKF 38393 (0922)
    SKF 83822 (2075)
    1
    3.2
    ~ 0.5
    3.1
    ~ 150
    186
    ~ 5000
    66
    ~ 1000
    335
    D1-like Antagonists SCH 23390 (0925) ~ 0.2 0.3 ~ 1100 ~ 800 ~ 3000
    D2-like Agonists Bromocriptine (0427)
    7-HydroxyDPAT (0706)
    Cabergoline (2664)
    ~ 440
    ~ 5000
    -
    ~ 450
    -
    165
    ~ 8
    10
    0.7
    ~ 5
    ~ 1
    1.5
    ~ 290
    650
    9.0
    D2-like Antagonists Clozapine (0444)
    Haloperidol (0931)
    Nemonapride (1746)
    NGB 2904 (2635)
    Raclopride (1810)
    Remoxipride (0916)
    Spiperone (0995)
    (S-(-)-Sulpride (0895)
    ~ 170
    ~ 80
    -
    > 10000
    18000
    -
    ~ 350
    ~ 45000
    ~ 330
    ~ 100
    -
    217
    -
    -
    ~ 3500
    77000
    ~ 230
    1.2
    0.06
    1.4
    1.8
    ~ 300
    0.06
    ~ 15
    ~ 170
    ~ 7
    0.3
    > 5000
    3.5
    ~ 1600
    0.6
    ~ 13
    21
    2.3
    0.15
    > 10000
    2400
    ~ 2800
    0.08
    1000
    All Ki values for agonists were determined at the high-affinity state for all receptors, except for D3 receptors.
    References
  • Seeman and Van Tol (1994) Dopamine receptor pharmacology. TiPS 15 264. Missale et al (1998) Dopamine receptors: from structure to function. Physiol.Rev. 78 189. O'Sullivan et al (2004) SK&F 83822 distinguishes adenylyl cyclase from phospholipase C-coupled D1-like receptors: behavioural topography. Eur.J.Pharmacol. 486 273. Kvernmo et al (2006) A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin.Ther. 28 1065. Yuan et al (1998) NGB 2904 and NGB 2849: two highly selective dopamine D3 receptor antagonists. Bioorg.Med.Chem.Lett. 8 2715.