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 제품안내  신경약학   Pharmacology

Adenosine Receptor Data

Adenosine Receptor agonist & antagonist를 소개합니다.

TOCRIS
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    Adenosine Receptor Data
    Receptor Subtype A1 A2A A2B A3
    Transduction Mechanism ↓Adenylyl Cyclase (Gi/o) and ↑ PLC ↑Adenylyl Cyclase (Gs) ↑Adenylyl Cyclase (Gs) and ↑ PLC (Gq) ↓Adenylyl Cyclase (Gi/o) and ↑ PLC
    Primary Distribution Brain (cortex, cerebellum, hippocampus), spinal cord, eye, adrenal gland, atria Spleen, thymus, leukocytes, platelets, striatopallidal GABAergic neurons, olfactory bulb Cecum, colon, bladder Testis, mast cells
    Tissue Function Antinociception, hypothermia, sedation, sleep, inhibition of lipolysis, cardio- and neuroprotection Reflex tachycardia, vasodilation, inhibition of platelet aggregation, sleep, protection against ischemia Relaxation of vascular and intestinal smooth muscle, cytokine production, inhibition of cell proliferation Mast cell degranulation, coronary vasodilation and protection from reperfusion

    Key Compounds Ki Values (nM)
    Agonists CGS 21680 (1063)
    2-Chloro-N6-cyclopentyladenosine (1705)
    2-Cl-IB-MECA (1104)
    N6-Cyclopentyladenosine (1702)
    HEMADO (1579)
    IB-MECA (1066)
    2'-MeCCPA (2281)
    NECA (1691)
    SDZ WAG 994 (2465)
    290
    0.8
    820 (rat)
    2.3
    327
    3.7
    3.3
    14
    23
    27
    2300
    470 (rat)
    790
    1230
    2500
    9580
    20 -
    88800*
    18800*
    -
    18600*
    100000*
    11000*
    37600
    2400*
    25000
    67
    42
    0.33 (rat)
    43
    1.1
    1.2
    1150
    6.2
    -
    Antagonists CGS 15943 (1699)
    DPCPX (0439)
    MRS 1220 (1217)
    MRS 1334 (1385)
    MRS 1706 (1584)
    MRS 1754 (2752)
    MRS 3777 (2403)
    PSB 36 (2019)
    SCH 442416 (2463)
    VUF 5574 (1359)
    ZM 241385 (1036)
    8-(3-Chlorostyryl)caffeine (3306)
    PSB 1115 (2009)
    PSB 603 (3198)
    3.5
    3.9
    305 (rat)
    > 100000 (rat)
    157
    403
    > 10000
    0.12 (rat)
    1111
    ~ 10000 (rat)
    540
    28200
    > 10000
    > 10000
    4.2
    130
    52 (rat)
    > 100000 (rat)
    112
    503
    > 10000
    552 (rat)
    0.048
    > 10000 (rat)
    1.4
    54
    24000
    > 10000
    16
    50
    -
    -
    1.39
    1.97
    > 10000
    187
    > 10000
    -
    31
    -
    53.4
    0.568
    51
    4000
    0.7
    5.69
    230
    570
    47
    2300
    > 10000
    4
    270
    -
    > 10000
    > 10000
    * EC50 values
    References
  • Klotz et al (2000) Naunyn-Schmied.Arch.Pharmacol. 362 382.Kim et al (1994) J.Med.Chem. 37 3614. van Muijlwijk-Koezen et al (2000) J.Med.Chem. 43 2227. Kim et al (2000) J.Med.Chem. 43 1165. Volpini et al (2002) J.Med.Chem. 45 3271. Li et al (1998) J.Med.Chem. 41 3186. Cappellacci et al (2005) J.Med.Chem. 48 1550. Osama et al (2004) J.Pharmacol.Exp.Ther. 308 358. Toddle et al (2000) J.Med.Chem. 43 4359. Jacobson and Gao (2000) Nat.Rev.Drug Discov. 5 247.