Kozhevnikova L M, Moskovtsev A A, Mesitov M V
Izv Akad Nauk Ser Biol. 2014 Sep-Oct(5):500-9.
We found that the inhibitor of Rho-kinase fasudil selectively inhibited constriction of isolated rings of the aorta and mesenteric artery in rats in response to application of the agonists of 5HT2A-(DOI and TBC-2) and 5HT1A-receptors (8-OH-DPAT) and did not influence vasoconstriction induced by serotonin. We demonstrate for the first time that application of the agonists of 5HT2C-receptors (MK 212 and SCH 23390) did not influence the tone of "intact" vessels. The marked vasoconstrictory effect of the agonists of 5HT2C-receptors was observed in the vessels preconstricted due to angiotensin II or vasopressin. We found that the inhibitor of Rho-kinase did not influence negatively on MK 212 or SCH 23390-induced constriction of isolated rings of the aorta and mesenteric artery in rats. We suppose.that, in the presence of fasudil, serotonin induces constriction of vessels through the interaction with 5HT2C-receptors and signal transduction from these receptors does not involve Rho-kinase activity. We found that fasudil attenuated vasoconstriction induced by norepinephrine and vasopressin by 40%. We.demonstrated that tyrosine c-Src-kinase plays the most important role in signal transduction from 5HT-receptors because its effects are specific with relation to these receptors.
我们发现，Rho激酶抑制剂法舒地尔可选择性抑制大鼠离体主动脉环和肠系膜动脉环对5HT2A受体激动剂（DOI和TBC-2）以及5HT1A受体激动剂（8-OH-DPAT）的收缩反应，且不影响血清素诱导的血管收缩。我们首次证明，应用5HT2C受体激动剂（MK 212和SCH 23390）对“完整”血管的张力无影响。在因血管紧张素II或血管加压素而预先收缩的血管中，观察到5HT2C受体激动剂具有明显的血管收缩作用。我们发现，Rho激酶抑制剂对MK 212或SCH 23390诱导的大鼠离体主动脉环和肠系膜动脉环收缩无负面影响。我们推测，在存在法舒地尔的情况下，血清素通过与5HT2C受体相互作用诱导血管收缩，且这些受体的信号转导不涉及Rho激酶活性。我们发现法舒地尔可使去甲肾上腺素和血管加压素诱导的血管收缩减弱40%。我们证明酪氨酸c-Src激酶在5HT受体的信号转导中起最重要作用，因为其作用对这些受体具有特异性。
