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Mechanism of hypotensive effects of verticillatine

  
@article{APS8567,
	author = {Bao-Hong Tian and Gui-Yun Zeng},
	title = {Mechanism of hypotensive effects of verticillatine},
	journal = {Acta Pharmacologica Sinica},
	volume = {9},
	number = {1},
	year = {2016},
	keywords = {},
	abstract = {Verticillatine (Vtc) is a new alkaloid first isolated in our institute from the water-soluble fraction of the root of Rauwolfia verricillata (Lour. ) Baill.      In anesthetized cats. iv Vtc 0.5-2.0 mg/kg produced dose-dependent ganglion blocking effects and the ED50 of blocking action on the sympathetic and parasympa-thetic  ganglion  were l.03 and  0.8 mg/kg. respectively. The affinity of Vtc to a-adrenoceptor was studied using radioligand binding assay in the rat brain cortex. The competitive curves showed that the apparent dissociation constant (Ki) of Vtc for ai and az-adrenoceptor were  0.22 and 0.11 pmol/L, respectively. Vtc antagonized NE-induced contraction of the rat anococcygeus and rabbit aorta (postsynaptic ai-adrenoceptor) and pAz value were 4.3 and 4.6, respectively. Vtc antagonized the inhibiting effects of clonidine on field stimulation twitch of the rat vas deferens (presynaptic az-adrenoceptor) and pAz value was 4.3.       Vtc and hexamethonium (Ca) manifested neither the central antihypertensive effect nor direct peripheral vasodilating action. C6 was found to be only a ganglionic blocking agent in this case. Vtc. in addition to its gangjion blocking action, showed a-adrenoceptor blocking properties.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/8567}
}