European Journal of Pharmacology: Molecular Pharmacology
Regular paperCoupling of human α2-adrenoceptor subtypes to regulation of cAMP production in transfected S115 cells
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Bidirectional effects of dexmedetomidine on human platelet functions in vitro
2015, European Journal of PharmacologyCitation Excerpt :P values less than 0.05 were considered to indicate statistical significance. Dexmedetomidine (50–2500 nM) enhanced platelet aggregation induced by 0.5 μM ADP in a dose-dependent manner, while levomedetomidine (2500 nM), an R (-)-enantiomer of medetomidine with an α2-adrenoceptor binding affinity much lower than that of dexmedetomidine (Jansson et al., 1994), had no significant effect (Fig. 1A). We next aimed to pharmacologically analyze which receptor is involved in the effect of dexmedetomidine on platelet aggregation.
High-throughput screening with a miniaturized radioligand competition assay identifies new modulators of human α<inf>2</inf>-adrenoceptors
2012, European Journal of Pharmaceutical SciencesCitation Excerpt :These receptors are encoded by three different intronless genes located on human chromosomes 10, 2 and 4, respectively (Kobilka et al., 1987; Lomasney et al., 1990; Regan et al., 1988). They mediate signals carried by the endogenous neurotransmitter noradrenaline and the hormone adrenaline to intracellular second messengers via pathways involving G proteins mainly of the Gi/o class, but also Gs and Gq proteins have been implicated in some of their cellular effects (Chabre et al., 1994; Conklin et al., 1992; Cotecchia et al., 1990; Eason et al., 1992; Jansson et al., 1994; Kurose et al., 1991; Pohjanoksa et al., 1997). α2-ARs mediate a wide spectrum of physiological functions and pharmacological effects.
Adrenal α<inf>2</inf>-adrenergic receptors in the aging normotensive and spontaneously hypertensive rat
2012, Neurobiology of AgingCitation Excerpt :The effect of the nicotinic receptor agonist 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP) on catecholamine release was determined by addition a single concentration of DMPP (500 μmol/L) delivered at t = 125 min. The inhibitory effect of the α2AR medetomidine (MED) on catecholamine release was determined by addition of a single concentration of MED (100 nmol/L) (Ki values in nM α2A: 0.8 ± 0.1; α2B: 3.8 ± 1.1; α2C: 8.8 ± 3.2) (Jansson et al., 1994). When used, the α-adrenergic receptor antagonist rauwolscine (300 nmol/L) was present from t = 90 min until the end of nicotinic stimulation.
Expression and characterization of the human α<inf>2B</inf>-adrenoceptor in a vascular smooth muscle cell line
2008, European Journal of PharmacologyEvaluation of the clinical efficacy and safety of dexmedetomidine or medetomidine in cats and their reversal with atipamezole
2006, Veterinary Anaesthesia and AnalgesiaCitation Excerpt :MED is a 1:1 racemic mixture of two optically active enantiomers of which only the d-isomer, dexmedetomidine (DEX), is pharmacologically active at clinically relevant doses (Virtanen et al. 1988; Savola & Virtanen 1991; Aantaa et al. 1993). The l-isomer, levomedetomidine, has been shown to be essentially inactive although in vitro studies have demonstrated that it may possess weak partial α2-adrenoceptor agonist or inverse α2-adrenoceptor agonist (negative antagonist) properties (Jansson et al. 1994, 1998). The pharmacodynamic effects of MED in dogs have been shown to be solely due to DEX while levomedetomidine is essentially inactive (Vickery et al. 1988; Kuusela et al. 2000, 2001).