比托特罗

比托特罗（INN：bitolterol）是一种短效β2肾上腺素受体激动剂，用于缓解哮喘^[1][2]和慢性阻塞性肺病等疾病的支气管痉挛。^[3][4][5]在这些疾病中，负责将空气输送到肺部的气道（支气管及其分支）会变窄。支气管内的肌肉痉挛和炎症加剧了这种变窄。比托特罗通过放松持续存在于支气管和支气管细支周围的平滑肌，有助于空气顺畅通过。

可尔特罗

比托特罗

临床资料
AHFS/Drugs.com	Micromedex详细消费者药物信息
MedlinePlus	a601236
ATC码	R03AC17 (WHO)
识别信息
IUPAC命名法 (RS)-[4-(1-Hydroxy-2-tert-butylamino-ethyl)-2-(4-methylbenzoyl)oxy-phenyl] 4-methylbenzoate
CAS号	30392-40-6 30392-41-7  Y
PubChem CID	35330
DrugBank	DB00901
ChemSpider	32525
UNII	9KY0QXD6LI mesylate: 4E53T3611U Y
ChEMBL	ChEMBL1201295 Y
CompTox Dashboard（英语：CompTox Chemicals Dashboard） (EPA)	DTXSID1022683
化学信息
化学式	C28H31NO5
摩尔质量	461.56 g·mol−1
3D模型（JSmol（英语：JSmol））	交互式图像
手性	外消旋混合物
SMILES O=C(Oc2cc(ccc2OC(=O)c1ccc(cc1)C)C(O)CNC(C)(C)C)c3ccc(cc3)C

比托特罗是可尔特罗的前药。^[6][7]它起效迅速（2至5分钟），可持续长达6至8小时。^[8]该药单独或与茶碱合用，不显示心脏毒性作用。^[9]

美国食品和药物管理局于1984年12月批准了比托特罗。该药物于2001年被Élan制药（英语：Élan）从市场上撤回。

参考资料

1. Nathan RA, Bodman SF, Storms WW, Mingo TS. Bitolterol mesylate aerosol in adults with steroid-dependent asthma: a comparison with isoproterenol hydrochloride aerosol. Annals of Allergy. June 1986, 56 (6): 494–499. PMID 3717716.
2. Nathan RA, Bernstein IL, Bronsky EA, Bush RK, Chervinsky P, Condemi JJ, et al. Comparison of the bronchodilator effects of nebulized bitolterol mesylate and isoproterenol hydrochloride in steroid-dependent asthma. The Journal of Allergy and Clinical Immunology. May 1987, 79 (5): 822–829. PMID 3571773. doi:10.1016/0091-6749(87)90216-8 .
3. Friedel HA, Brogden RN. Bitolterol. A preliminary review of its pharmacological properties and therapeutic efficacy in reversible obstructive airways disease. Drugs. January 1988, 35 (1): 22–41. PMID 3278878. S2CID 218471864. doi:10.2165/00003495-198835010-00002. （原始内容存档于2012-12-23）.
4. Early Career Awards for 1978 (John Robert Anderson, Philip M. Groves, Gary E. Schwartz). The American Psychologist. January 1979, 34 (1): 69–79. PMID 396832. doi:10.1037/h0078247.
5. Petty TL, Scoggin CH, Rollins DR, Repsher LH. Bitolterol compared to isoproterenol in advanced chronic obstructive pulmonary disease. Chest. September 1984, 86 (3): 404–408. PMID 6380974. doi:10.1378/chest.86.3.404.
6. Walker SB, Kradjan WA, Bierman CW. Bitolterol mesylate: a beta-adrenergic agent. Chemistry, pharmacokinetics, pharmacodynamics, adverse effects and clinical efficacy in asthma. Pharmacotherapy. 6 May 1985, 5 (3): 127–137. PMID 3895171. S2CID 29431526. doi:10.1002/j.1875-9114.1985.tb03410.x.
7. ChEBI: Bitolterol. Chemical Entities of Biological Interest. Wellcome Genome Campus, Hinxton, Cambridgeshire, CB10 1SD, UK. [27 March 2016]. （原始内容存档于2024-03-28）.
8. Kass I, Mingo TS. Bitolterol mesylate (WIN 32784) aerosol. A new long-acting bronchodilator with reduced chronotropic effects. Chest. August 1980, 78 (2): 283–287. PMID 6995040. doi:10.1378/chest.78.2.283.
9. Kemp JP, Chervinsky P, Orgel HA, Meltzer EO, Noyes JH, Mingo TS. Concomitant bitolterol mesylate aerosol and theophylline for asthma therapy, with 24 hr electrocardiographic monitoring. The Journal of Allergy and Clinical Immunology. January 1984, 73 (1 Pt 1): 32–43. PMID 6693665. doi:10.1016/0091-6749(84)90481-0 .