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HOKU-81

Names

[ CAS No. ]:
58020-43-2

[ Name ]:
HOKU-81

[Synonym ]:
2-tert-butylfluorenone
2-tert.-Butylfluorenon
2-tert-butyl-9-fluorenone

Biological Activity

[Description]:

HOKU-81, a new bronchodilator, is one of the metabolites of tulobuterol. IC50 Value: Target: Adrenergic ReceptorEffects of HOKU-81 on isolated trachea and atria of guinea pigs were compared with those of various bronchodilators. HOKU-81 appears to be a potent and selective beta 2-stimulant with a slight inotropic action. HOKU-81 was approximately 8 times more potent than tulobuterol, approximately twice as potent as salbutamol, and approximately as potent as isoprenaline in relaxing effect on the isolated tracheal smooth muscle preparation of guinea pigs. This effect of HOKU-81 seems to be due to direct action on the adrenergic beta-receptor.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Cardiovascular Disease

[References]

[1]. Kubo S, Matsubara I, Yamazaki M et al. Pharmacological studies of 1-(2-chloro-4-hydroxyphenyl)-2-t-butylaminoethanol (HOKU-81), a new bronchodilator. 1st Communication: Bronchodilator and cardiovascular actions. Arzneimittelforschung. 1980;30(8):1272-8.

[2]. Gomi Y, Shirahase H, Funato H. Effects of 1-(2-chloro-4-hydroxyphenyl)-t-butylaminoethanol (HOKU-81), a new bronchodilator, on isolated trachea and atria of guinea pig. Jpn J Pharmacol. 1979 Aug;29(4):515-24.


[Related Small Molecules]

Isoprenaline hydrochloride | ICI 118,551 (hydrochloride) | Phenylephrine hydrochloride | Yohimbine hydrochloride | Adrenaline | Ivabradine hydrochloride | Prazosin hydrochloride | Clenbuterol hydrochloride | Phentolamine mesilate | guanfacine hydrochloride | pimozide | Sotalol hydrochloride | Carvedilol | Atenolol | Metroprolol succinate

Chemical & Physical Properties

[ Density]:
1.184g/cm3

[ Boiling Point ]:
392ºC at 760mmHg

[ Molecular Formula ]:
C12H18ClNO2

[ Molecular Weight ]:
243.73000

[ Flash Point ]:
190.9ºC

[ Exact Mass ]:
243.10300

[ PSA ]:
52.49000

[ LogP ]:
2.85800

[ Index of Refraction ]:
1.556

[ Storage condition ]:
2-8℃


Related Compounds