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• W2021351279 abstract "1 In the present study, depletion of internal Ca2+ stores sensitive to noradrenaline (1 μm) in rat aorta, is the signal for the entry of extracellular Ca2+, not only to refill the stores but also, in our experimental conditions, to activate the contractile proteins. This induces an increase in the resting tone that constitutes, the first functional evidence of this Ca2+ entry. 2 The fact that methoxamine (100 μm) reproduces the same processes as noradrenaline but clonidine (1 μm) does not, indicates that α1-adrenoceptor activation is related to the increase in the resting tone observed after depletion of adrenoceptor-sensitive internal Ca2+-stores. 3 Benoxathian and WB 4101 (α1A- and α1D-adrenoceptor antagonists) selectively inhibit, in a concentration-dependent manner, this mechanical response observed in absence of the agonist, which suggests that these agents can act as inverse agonists and provide a functional model for studying this phenomenon. Since chloroethylclonidine (100 μm) has no effect on this response, the participation of α1B-adrenoceptors can be ruled out. 4 Contractile responses to noradrenaline (1 μm) in Ca2+-free medium were selectively blocked by chloroethylclonidine. This suggests that the response to noradrenaline in Ca2+-free medium mainly depends on the activation of the α1B-adrenoceptor subtype." @default.
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• W2021351279 date "1996-09-01" @default.
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• W2021351279 title "Functional evidence of inverse agonism in vascular smooth muscle" @default.
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• W2021351279 doi "https://doi.org/10.1111/j.1476-5381.1996.tb15689.x" @default.
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