盐酸吲哚拉明（Wy 21901）自主神经阻滞特性的离体器官定量分析。
Quantitative analysis on isolated organs of the autonomic blocking properties of indoramin hydrochloride (Wy 21901).
作者信息
Alps B J, Hill M, Johnson E S, Wilson A B
出版信息
Br J Pharmacol. 1972 Jan;44(1):52-62. doi: 10.1111/j.1476-5381.1972.tb07237.x.
Abstract
- Indoramin is a competitive alpha-adrenoceptor blocking agent on the guinea-pig isolated vas deferens and aortic strip; the pA(2) value on the aorta is 7.4.2. Indoramin is devoid of beta-adrenoceptor blocking activity on the guinea-pig isolated trachea (10(-4)M) and the Langendorff preparation of the rabbit heart (10(-6)M). It also has no adrenergic neurone blocking action on the Finkleman preparation of the rabbit small intestine (10(-5)M).3. On the Langendorff preparation of the rabbit isolated heart, indoramin (above 10(-6)M) has cardio-inhibitory properties similar to those of propranolol.4. On the guinea-pig isolated ileum (10(-5)M) and trachea (10(-6)M), indoramin is devoid of anticholinergic activity, but has a potent antihistamine action which satisfies the criteria for competitive antagonism; the pA(2) value for this antagonism on the ileum is 8.2.5. Indoramin antagonizes 5-hydroxytryptamine on the rat isolated fundus and ileum; the pA(2) value for the antagonism on the ileum is 6.0.
摘要
吲哚拉明是豚鼠离体输精管和主动脉条上的竞争性α-肾上腺素能受体阻断剂；在主动脉上的pA(2)值为7.4。
吲哚拉明对豚鼠离体气管（10⁻⁴M）和兔心脏Langendorff标本（10⁻⁶M）无β-肾上腺素能受体阻断活性。它对兔小肠Finkleman标本（10⁻⁵M）也无肾上腺素能神经元阻断作用。
在兔离体心脏Langendorff标本上，吲哚拉明（高于10⁻⁶M）具有与普萘洛尔相似的心脏抑制特性。
在豚鼠离体回肠（10⁻⁵M）和气管（10⁻⁶M）上，吲哚拉明无抗胆碱能活性，但具有强效的抗组胺作用，符合竞争性拮抗的标准；在回肠上这种拮抗作用的pA(2)值为8.2。
吲哚拉明在大鼠离体胃底和回肠上拮抗5-羟色胺；在回肠上这种拮抗作用的pA(2)值为6.0。
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