A racemic mixture of of L-norepinephrine and D-norepinephrine
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(±)-Norepinephrine is a racemic mixture of the endogenous neurotransmitter (–)-norepinephrine and (+)-norepinephrine. It induces cAMP accumulation in rat cerebral cortical membranes when used at concentrations ranging from 1 to 100 ?M.1 (±)-Norepinephrine induces contraction of bovine anterior cerebral, middle cerebral, and internal carotid arterial strips (EC50s = 0.91, 0.92, and 0.87 ?M, respectively) but induces relaxation of bovine posterior cerebral arterial strips (EC50 = 0.95 ?M).2
1.Tadokoro, C., Kiuchi, Y., Yamazaki, Y., et al.Behavioral stimulation without alteration of β and 5-HT receptors and adenylate cyclase activity in rat brain after chronic sertraline administrationPsychopharmacology (Berl.)130(2)124-130(1997) 2.Ayajiki, K., and Toda, N.Isolated bovine cerebral arteries from rostral and caudal regions: Distinct responses to adrenoceptor agonistsEur. J. Pharmacol.191(3)417-425(1990)
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Cell experiment: |
Subcutaneous preadipocytes derived from a 38-year old non-diabetic female donor are immortalized with TERT and HPV E6/E7. For the current studies, a stable diploid clone (referred to as clone B) with consistent differentiation capacity is isolated by ring cloning. Cells are grown in preadipocyte PGM2 media. Once cells are confluent, differentiation is induced by incubation in differentiation media consisting of dexamethasone, IBMX, indomethacin, and additional insulin. Cells are differentiated for 10 days. Prior to treatment, media is replaced with PGM2 media for one day and then switched to serum-free media overnight for treatments. Adipocytes are treated for 6 hours with vehicle, Norepinephrine (NE, 10 μM), CGP (10 nM), or Norepinephrine (NE) and CGP[2]. |
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参考文献: [1]. MacGregor DA, et al. Relative efficacy and potency of beta-adrenoceptor agonists for generating cAMP in human lymphocytes. Chest. 1996 Jan;109(1):194-200. |
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