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Chemical Compound Review:

Tibalosin 1-(2,3-dihydrobenzothiophen- 5-yl)-2-(4...

Synonyms: SureCN1254588, AC1L4SDC, AR-1I2736, KB-212541, AC1Q3F37, ...

This record was replaced with 163028.

Staessen, J. et al., Staessen, J. et al., Qian, J.Q. et al., Chatelain, P. et al., Staessen, J. et al., et al.

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Disease relevance of 1-(2,3-dihydrobenzothiophen-5-yl)-2-(4-phenylbutylamino)propan-1-ol

Effects of tibalosine, a new alpha-adrenoceptor antagonist, in essential hypertension [1].

High impact information on 1-(2,3-dihydrobenzothiophen-5-yl)-2-(4-phenylbutylamino)propan-1-ol

Standing (-5.5/-6.0 mm Hg) and supine (-8.5/-7.5 mm Hg) blood pressure and standing (-7.0 bmp) and supine (-7.5 bpm) pulse rate were reduced by tibalosine [1].
In conclusion tibalosine reduced blood pressure at rest and during exercise independently of opioidergic mechanisms [2].
On tibalosine their blood pressure decreased from 157/101 to 147/93 mm Hg (p less than 0.001) and their heart rate from 74 to 68 beats per minute (p less than 0.01), while plasma renin activity tended to fall from 0.81 to 0.65 ng/ml/hr (p = 0.06) [3].
Tibalosine interacts specifically with alpha- and beta-adrenergic receptors and calcium channel binding sites [4].
Tibalosine and CP 804 S/T interact with the low affinity binding sites labelled by 3H-WB 4101 in rat brain membranes [4].

Associations of 1-(2,3-dihydrobenzothiophen-5-yl)-2-(4-phenylbutylamino)propan-1-ol with other chemical compounds

As compared to tibalosine plus placebo, blood pressure and heart rate decreased further on tibalosine plus atenolol from 148/97 to 140/90 mm Hg (p less than 0.05) and from 70 to 60 beats per minute (p less than 0.05), respectively [3].
In pithed normotensive rats, tibalosine inhibited the pressor responses to i.v. cirazoline (pA2 = 5.47 +/- 0.17), but not to those by i.v. B-HT 920 Tibalosine selectively displaced [3H]-prazosin from its specific binding site in rat isolated brain membranes [5].

Analytical, diagnostic and therapeutic context of 1-(2,3-dihydrobenzothiophen-5-yl)-2-(4-phenylbutylamino)propan-1-ol

In a double-blind cross-over study, 12 patients with essential hypertension, on a constant sodium intake, received placebo and tibalosine, 150 mg daily [1].
CP-804-S is a substituted phenylbutylamine, known to lower arterial pressure in hypertensive animal models [6].

References

Effects of tibalosine, a new alpha-adrenoceptor antagonist, in essential hypertension. Staessen, J., Fagard, R., Grauwels, R., Lijnen, P., Verschueren, L.J., Amery, A. Clin. Pharmacol. Ther. (1983) [Pubmed]
Alpha-adrenoceptor blockade by tibalosine: hemodynamic and humoral effects at rest and during exercise, and effect of opioid receptor antagonism. Staessen, J., Fiocchi, R., Fagard, R., Lijnen, P., Amery, A. J. Cardiovasc. Pharmacol. (1986) [Pubmed]
Chronic treatment with tibalosine in essential hypertension. Staessen, J., Fagard, R., Fiocchi, R., Lijnen, P., M'Buyamba-Kabangu, J.R., Amery, A. Archives internationales de pharmacodynamie et de thérapie. (1986) [Pubmed]
Receptor binding profile of tibalosine, a new antihypertensive. Chatelain, P., Friedhoff, A.J., Meller, E., Mennini, T., Gorissen, H., Roba, J. Arzneimittel-Forschung. (1984) [Pubmed]
Antihypertensive activity and interaction with alpha-adrenoceptors of tibalosine ([1-(2, 3-dihydro-5-benzo-(b)-thienyl)-2-(4-phenyl-butylamino)-1-propanol], CP 804 S) in rat and cat preparations. Qian, J.Q., Mathy, M.J., Thoolen, M.J., Timmermans, P.B., van Zwieten, P.A. Archives internationales de pharmacodynamie et de thérapie. (1983) [Pubmed]
Influence of central alpha 1 inhibition in patients with essential hypertension. Lijnen, P., Staessen, J., Fagard, R., Amery, A. Chest (1983) [Pubmed]

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