Penbutolol sulfate ((-)-Terbuclomine)

A β-adrenergic and 5-HT1A receptor antagonist

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10mg

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货号: ajce49230
CAS: 38363-32-5
别名: 喷布特罗硫酸盐,(-)-Terbuclomine
分子式: C18H29NO2 . 1/2 H2O4S
分子量: 340.47
纯度: >98%
溶解度: Water : 5 mg/mL (14.69 mM)
储存: Store at -20°C,sealed storage, away from moisture
库存: 现货

Background

Penbutolol is an antagonist of β-adrenergic receptors (β-ARs; IC₅₀ = 2.8 nM) and the serotonin (5-HT) receptor subtype 5-HT_1A (IC₅₀ = 9.9 nM).¹ It inhibits adenylate cyclase activity induced by the β-AR agonist isoprenaline in guinea pig myocardial membranes with a K_i value of 2.4 nM.² Penbutolol reduces basal renin activity and blood pressure in spontaneously hypertonic rats.³ It decreases isolation-induced aggressive behavior in mice (ED₅₀ = 56 ?mol/kg) and reverses reductions in aggression induced by 8-hydroxy-DPAT and TFMPP with ED₅₀ values of 8.1 and 2.1 ?mol/kg, respectively.¹ Formulations containing penbutolol were previously used in the treatment of arterial hypertension.

1.Sánchez, C., Arnt, J., and Moltzen, E.K.The antiaggressive potency of (–)-penbutolol involves both 5-HT1A and 5-HT1B receptors and β-adrenoceptorsEur. J. Pharmacol.297(1-2)1-8(1996) 2.Krawietz, W., Poppert, D., Erdmann, E., et al.β-adrenergic receptors in guinea-pig myocardial tissueNaunyn Schmiedebergs Arch. Pharmacol.295(3)215-224(1976) 3.Kaiser, J., H?rtfelder, G., Lindner, E., et al.Pharmacology of the β-receptor blocker penbutololArzneimittelforschung30(3)420-427(1980)