Chang F W, Burke J A, Potter D E
Department of Pharmacology, Texas Tech University Health Sciences Center, Lubbock.
J Ocul Pharmacol. 1985 Summer;1(2):137-47. doi: 10.1089/jop.1985.1.137.
Ketanserin has been characterized as a relatively selective antagonist for serotonin (5-HT2) receptors. However, recent evidence suggests that ketanserin can also antagonize activity at alpha 1-adrenoceptors. Topically applied ketanserin lowered intraocular pressure (IOP) in rabbits, cats, and monkeys. Ketanserin also suppressed ocular hypertension induced by waterloading and the IOP recovery rate in response to hypertonic saline. In contrast, the ocular hypotensive activity of ketanserin was markedly attenuated in sympathectomized (SX) rabbits. In the cat nictitating membrane, ketanserin produced dose-related inhibition of contractions elicited by neuronal stimulation and by intra-arterial injection of norepinephrine. These data demonstrate that ketanserin: 1) lowers IOP more effectively in eyes with intact sympathetic innervation than in SX eyes, 2) appears to lower IOP by suppressing aqueous inflow, and 3) acts primarily by antagonizing the action of norepinephrine on alpha 1-adrenoceptors.
酮色林已被表征为一种相对选择性的5-羟色胺（5-HT2）受体拮抗剂。然而，最近的证据表明，酮色林也能拮抗α1-肾上腺素能受体的活性。局部应用酮色林可降低兔、猫和猴的眼压（IOP）。酮色林还可抑制水负荷诱导的高眼压以及对高渗盐水的眼压恢复率。相反，在去交感神经（SX）的兔中，酮色林的降眼压活性明显减弱。在猫的瞬膜中，酮色林对神经刺激和动脉内注射去甲肾上腺素引起的收缩产生剂量相关的抑制作用。这些数据表明：1）与SX眼相比，酮色林在交感神经支配完整的眼中能更有效地降低眼压；2）似乎通过抑制房水流入来降低眼压；3）主要通过拮抗去甲肾上腺素对α1-肾上腺素能受体的作用发挥作用。
