西拉唑啉
化合物
西拉唑啉(INN:cirazoline)是α1A肾上腺素受体的完全激动剂、α1B和α1D肾上腺素受体的部分激动剂[1]以及α2肾上腺素受体的非选择性拮抗剂。[2]据信,这种特性的组合可以使西拉唑啉成为有效的血管收缩剂。[2]
西拉唑啉 | |
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IUPAC名 2-[(2-Cyclopropylphenoxy)methyl]-4,5-dihydro-1H-imidazole | |
识别 | |
CAS号 | 59939-16-1 |
PubChem | 2765 |
ChemSpider | 2663 |
SMILES |
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InChI |
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InChIKey | YAORIDZYZDUZCM-UHFFFAOYAV |
MeSH | Cirazoline |
IUPHAR配体 | 515 |
性质 | |
化学式 | C13H16N2O |
摩尔质量 | 216.279 g/mol g·mol⁻¹ |
若非注明,所有数据均出自标准状态(25 ℃,100 kPa)下。 |
据称,西拉唑啉还可以通过激活大脑下丘脑室旁核中的α1肾上腺素受体来减少大鼠的食物摄入量。[3]服用西拉唑啉似乎还会通过激活相同的受体来损害猴子的空间记忆。[4][5]然而,在初步研究中,通过刺激α2肾上腺素受体,工作记忆得到了相对改善。[4]
参考资料
- ^ Horie, K; Obika, K; Foglar, R. Selectivity of the imidazoline α-adrenoceptor agonists (oxymetazoline and cirazoline) for human cloned α1-adrenoceptor subtypes. British Journal of Pharmacology. 1995, 116 (1): 1611–8. PMC 1908909 . PMID 8564227. doi:10.1111/j.1476-5381.1995.tb16381.x.
- ^ 2.0 2.1 Ruffolo, R. R. Jr.; Waddell, J. E. Receptor interactions of imidazolines. IX. Cirazoline is an α1 adrenergic agonist and an α2 adrenergic antagonist. Journal of Pharmacology and Experimental Therapeutics. 1982, 222 (1): 29–36. PMID 6123592.
- ^ Davies, B. T.; Wellman, P. J. Effects on ingestive behavior in rats of the α1-adrenoceptor agonist cirazoline. European Journal of Pharmacology. 1992, 210 (1): 11–16. PMID 1350985. doi:10.1016/0014-2999(92)90645-K.
- ^ 4.0 4.1 Arnsten, A.F.T.; Jentsch, J.D. The Alpha-1 Adrenergic Agonist, Cirazoline, Impairs Spatial Working Memory Performance in Aged Monkeys. Pharmacology Biochemistry and Behavior. September 1997, 58 (1): 55–59. ISSN 0091-3057. PMID 9264070. S2CID 20663570. doi:10.1016/s0091-3057(96)00477-7 .
- ^ Imbery, Irdmusa, Speidell, Streer, Griffin, Ted E., Mitra S., Andrew P., Mark S., John D. The effects of Cirazoline, an alpha-1 adrenoreceptor agonist, on the firing rates of thermally classified anterior hypothalamic neurons in rat brain slices. Brain Research. 15 December 2007, 1193: 93–101. PMC 2268753 . PMID 18184607. doi:10.1016/j.brainres.2007.12.016.