Tatsui Sonoko, Ishikawa Hitoshi, Shimizu Kimiya, Mashimo Kimiyo
Department of Ophthalmology, School of Medicine, Kitasato University, Sagamihara, Japan.
Department of Orthoptics and Visual Sciences, School of Allied Health Sciences, Kitasato University, Sagamihara, Japan.
Clin Ophthalmol. 2016 May 11;10:845-9. doi: 10.2147/OPTH.S100755. eCollection 2016.
Brimonidine is an imidazoline compound used for the treatment of glaucoma, but having very little effect on pupil diameter. Like para-aminoclonidine, most imidazoline compounds interact with postsynaptic α-adrenoceptors and cause pupil dilatation. Therefore, as part of an investigation of the mechanism of action of brimonidine on pupil diameter, the present study was initiated to measure, in vitro, the relative potency of brimonidine on the pre- and postsynaptic α-adrenoceptors of rabbit iris dilator muscle.
The contractile activity of brimonidine and its effect on twitch contraction evoked by electrical field stimulation were studied in isolated rabbit iris dilator muscles by isometric tension recording.
Brimonidine significantly inhibited the twitch contraction of the dilator muscle caused by field stimulation, without affecting the response to exogenously applied phenylephrine. Compared to phenylephrine, brimonidine caused only a small contractile response with % maximum contraction values of <10%.
These results suggest that brimonidine may act on nerve endings to inhibit adrenergic neurotransmission with very little effect on postsynaptic α-adrenoceptors. This may indicate that brimonidine reduced the pupil diameter just a little, thus improving night vision.
溴莫尼定是一种用于治疗青光眼的咪唑啉化合物,但对瞳孔直径影响极小。与对氨基可乐定一样,大多数咪唑啉化合物与突触后α-肾上腺素能受体相互作用并导致瞳孔扩张。因此,作为对溴莫尼定对瞳孔直径作用机制研究的一部分,本研究旨在体外测量溴莫尼定对兔虹膜开大肌突触前和突触后α-肾上腺素能受体的相对效力。
通过等长张力记录,研究溴莫尼定在离体兔虹膜开大肌中的收缩活性及其对电场刺激诱发的抽搐收缩的影响。
溴莫尼定显著抑制电场刺激引起的开大肌抽搐收缩,而不影响对外源性去氧肾上腺素的反应。与去氧肾上腺素相比,溴莫尼定仅引起小的收缩反应,最大收缩值百分比<10%。
这些结果表明,溴莫尼定可能作用于神经末梢以抑制肾上腺素能神经传递,而对突触后α-肾上腺素能受体影响极小。这可能表明溴莫尼定仅略微减小瞳孔直径,从而改善夜间视力。