• Home
  • About us
  • Log-In
  • Join Us
  • Sitemap
  • Recruit
제품/실험 Q&A
자주묻는질문
자유게시판
실험기법
자료신청
논문자료
클레임 접수
기기 A/S 접수
클레임 진행조회
 제품안내  신경약학   Pharmacology

Cannabinoid Receptor

Cannabinoid Receptor agonist & antagonist를 소개합니다.

TOCRIS
제품 문의하기
인쇄하기

    Cannabinoid Receptor Data
    Receptor Subtype CB1 CB2 GPR55
    Transduction Mechanism ↓Adenylyl Cyclase (Gi/o), ↓ N- and P/Q-type Ca2+ currents, ↑ Kir and A-types K+ currents ↓ Adenylyl Cyclase (Gi/o) Activation of Rho family GTPases
    Primary Distribution CNS: hippocampus, basal ganglia, cerebellum, cortex, globus pallidus, substantia nigra, pars reticulata Spleen, tonsils, immune cells CNS: caudate and putamen
    Tissue Function Modulation of neurotransmitter release Suppression of immune cell function Pain signaling, control of vascular tone, inflammation

    Key Compounds Ki Values (nM) at CB1 Ki Values (nM) at CB2
    Endogenous Agonists Anandamide (1339)
    2-Arachidonylglycerol (1298)
    NADA (1568)
    Noladin ether (1411)
    61-543
    58.3-472
    2501
    21.2
    279-1940
    145-1400
    12001
    > 3000
    Key CB1 Agonists ACEA (1319)
    ACPA (1318)
    (R)-(+)-Methanandamide (1121)
    1.4
    2.2
    17.9-28.3
    > 2000
    715
    815-868
    Key CB2 Agonists CB 65 (2663)
    GP 1a (2764)
    GP 2a (2678)
    GW 405833 (2374)*
    JWH 015 (1341)
    JWH 133 (1343)
    L-759,656 (2434)
    L-759,633 (2433)
    > 1000
    363
    900
    4772
    383
    677
    4888
    1043
    3.3
    0.037
    7.6
    3.92
    13.8
    3.4
    11.8
    6.4
    Non-selective Agonists CP 55,940 (0949)
    HU 210 (0966)
    O-2545 (2680)
    WIN 55,212-2 (1038)
    Bay 59-3074 (2500)
    Δ9-Tetrahydrocannabinol (2741)
    0.5-5.0
    0.06-0.73
    1.5
    5.05
    1.89-123
    48.3
    5.05
    0.69-2.8
    0.17-0.52
    0.32
    3.13
    0.28-16.2
    45.5
    3.13
    Key CB1 Antagonists/
    Inverse Agonists
    AM 251 (1117)
    AM 281 (1115)
    LY 320135 (2387)
    7.49
    12
    141
    2290
    4200
    14900
    Key CB1 Antagonists/
    Inverse Agonists
    AM 630 (1120) 5152 31.2
    References
  • Bisogno et al (2000) N-acyl-dopamines: novel synthetic CB1 cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimimetic activity in vitro and in vivo. Biochem.J. 351 817. Pertwee (2006) Cannabinoid receptor ligands. Tocris Reviews No. 27.Manera et al (2006) Design, synthesis, and biological evaluation of new 1,8-naphthyridin-4(1H)-on-3-carboxamide and quinolin-4(1H)-on-3-carboxamide derivatives as CB2 selective agonists. J.Med.Chem. 49 5947. Murineddu et al (2006) Tricyclic pyrazoles. 4. Synthesis and biological evaluation of analogues of the robust and selective CB2 cannabinoid ligand 1-(2',4'-dichlorophenyl)-6-methyl-N-piperidin-1-yl-1,4-dihydroindeno[1,2-c]pyrazole-3-carboxamide. J.Med.Chem. 49 7502. Ross et al (1999) Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. Br.J.Pharmacol. 126 665. Martin et al (2006) Pharmacological characterization of novel water-soluble cannabinoids. J.Pharmacol.Exp.Ther. 318 1230. Pertwee (2008) The diverse CB1 and CB2 receptor pharmacology of three plant cannabinoids: Δ9-tetrahydrocannabinol, cannabidiol and Δ9-tetrahydrocannabivarin. Br.J.Pharmacol. 153 199.