MUDr. Dana Maňasková


Vyhledávání na medicinman.cz
 

Antagonisticky působící látky a vlivy

Beta3-adrenoceptor knockout mice

  • In BAT of beta3-adrenoceptor knockout mice
    • The beta1- and beta2-responses were fully conserved
  • Absence of response to CL 316,243
    • Beta4-adrenoceptor is present in BAT ? [7]
  • Associated with significantly increased urine excretion of water, sodium, potassium, and chloride [8]




L-748,337

  • Selective beta3 antagonist [4]
  • Chemical Name: N-[[3-[(2S)-2-Hydroxy-3-[[2-[4-[(phenylsulfonyl)amino]phenyl]ethyl]amino]propoxy]phenyl]methyl]-acetamide
  • Competitive beta3-adrenoceptor antagonist that displays selectivity over beta1 and beta2 receptors
    • (Ki values are 4.0, 204 and 390 nM for beta3-, beta2- and beta1-adrenoceptors respectively)
  • Inhibits cAMP accumulation in response to isoproterenol (IC50 = 6 nM)
  • Reduces iNOS expression, attenuates nitric oxide-induced cell proliferation and induces apoptosis in a melanoma cell line [4]
  • Formula C26H31N3O5S
  • Candelore et al (1999)
    • Potent and selective human beta3-adrenergic receptor antagonist. J.Pharmacol.Exp.Ther. 290 649 PMID: 10411574
  • Neidhold et al (2007)
    • The function of alpha - and beta-adrenoceptors of the saphenous artery in caveolin-1 knockout and wild-type mice. Br.J.Pharmacol. 150 261 PMID: 17179950
  • Dal Monte et al (2014)
    • Beta3-adrenergic receptor activity modulates melanoma cell proliferation and survival through nitric oxide signaling. Naunyn Schmiedebergs Arch.Pharmacol. 387 533 PMID: 24599317 [4]

SR 59230A hydrochloride

  • Potent and selective beta3 antagonist [4]
    • (IC50 values are 40, 408 and 648 nM for beta 3, beta 1 and beta 2 receptors respectively)
  • Chemical Name: 1-(2-Ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-(2S)-2-propanol hydrochloride
  • Orally active in vivo.
  • Formula C21H27NO2.HCl
  • Manara et al (1996)
    • Functional identification of rat atypical beta -adrenoceptors by the first beta 3-selective antagonists, aryloxypropanolaminotetralins. Br.J.Pharmacol. 117 435 PMID: 8821531
  • Mizuno et al (2002)
    • Stimulation of beta 3-adrenoceptors causes phosphorylation of p38 mitogen-activated protein kinase via a stimulatory G protein-dependent pathway in 3T3-L1 adipocytes. Br.J.Pharmacol. 135 951 PMID: 11861323
  • Manara et al (1995)
    • Aryloxypropanolaminotetralins are the first selective antagonists for atypical (beta 3) beta -adrenoceptors. Pharmacol.Comm. 6 253 [4]

O úroveň výše

Poslední aktualizace: 2. 1. 2019 16:25:14