Caroverine hydrochloride 是一种有效，竞争性和可逆的 NMDA 和 AMPA 谷氨酸受体拮抗剂。Caroverine hydrochloride 也是一种抗氧化剂和钙阻断剂，具有血管舒张作用。Caroverine hydrochloride 可用于内耳耳鸣的研究。
Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus[1][2][3].
Caroverine (1 μM; pretreated for 10 min) inhibits the pressor response to KCl (80 mM) and noradrenaline (1 μM) in the rat hindquarter preparation. Caroverine markedly suppresses the contraction caused by KCl (40 mM) in the rat isolated aorta[3].
Caroverine (1.44 mg/rat; s.c; 1.0 mL/h for 72 h) attenuates impulse noise-induced hearing loss in the rat[4].
参考文献:
[1]. Chen Z, et, al. Pharmacokinetics of caroverine in the inner ear and its effects on cochlear function after systemic and local administrations in Guinea pigs. Audiol Neurootol. Jan-Feb 2003;8(1):49-56.
[2]. Denk DM, et, al. Caroverine in tinnitus treatment. A placebo-controlled blind study. Acta Otolaryngol. 1997 Nov;117(6):825-30.
[3]. Ishida Y, et, al. Vasorelaxant action of caroverine fumarate (a quinoxaline derivative), a calcium-blocking agent. Br J Pharmacol. 1980;71(1):343-8.
[4]. Duan M, et, al. Low-dose, long-term caroverine administration attenuates impulse noise-induced hearing loss in the rat. Acta Otolaryngol. 2006 Dec;126(11):1140-7.
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