Pharmacologic profile of urapidil

Zwieten, P. A. van

doi:10.1016/0002-9149(89)90687-5

Cited by 19 publications

(5 citation statements)

References 25 publications

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“…13 The initial effect, occurring shortly after injection, seems to be a vasodilation with more pronounced effects in SHR than in WKY rat strains. The induced fall in blood pressure was not associated with a change in cardiac output or heart rate in either strain, suggesting an inhibition of the baroreceptor reflex response to arteriolar vasodilation.…”

Section: Discussionmentioning

confidence: 99%

“…This central mechanism, distinct from that of clonidine, could involve a 5-hydroxytryptamine agonistic potency. 13 In the present investigation, the antihypertensive effect of intravenous Urapidil was studied in normotensive Wistar-Kyoto (WKY) rats and spontaneously hypertensive rats (SHR). To specifically investigate the direct effects of Urapidil on the arterial wall properties, the static mechanical properties of the carotid arterial wall were also measured after local incubation with Urapidil.…”

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confidence: 99%

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Effects of alpha 1-blockade on arterial compliance in normotensive and hypertensive rats.

1991

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The effects of blockade of cq-adrenergic receptors on the mechanical properties of the arterial wall were studied in 10 spontaneously hypertensive rats (SHR) as compared with 10 matched normotensive Wistar-Kyoto (WKY) rats. Ascending aortic pressure and flow were recorded in open-chest anesthetized rats, and the systemic arterial compliance was calculated. Intravenous injection (1 mg/kg) of Urapidil, a selective «,-adrenergic antagonist, induced a significant decrease in arterial pressure (-26%, p<0.01 and -37%, p<0.001 in WKY rats and SHR, respectively) without significant changes in cardiac output. In control conditions, systemic arterial compliance was lower in SHR (3.29 ±1.52 /il/mm Hg) than in WKY rats ( 4 J 5 ± U 5 fil/mm Hg, p<0.01). Urapidil injection induced significant increases in systemic arterial compliance values in both strains (p<0.001). In another set of experiments (15 WKY rats and 15 SHR), the carotid compliance (filjmm Hg) was determined from the arterial volumepressure relation under control conditions, after local incubation with Urapidil, and after total abolition of the vascular smooth muscle by KCN. In WKY rats, the carotid compliance increased markedly after incubation with Urapidil at doses corresponding to 1 mg/kg (+31%, p<0.01). A further increase in the carotid compliance was observed after KCN poisoning (+11%, p<0.05). In SHR, incubation with Urapidil at doses corresponding to 2 mg/kg were necessary to induce a significant increase in compliance (+38%). At this dosage, there was no further increase in compliance after KCN poisoning. The present study suggests that (^blockade influences the arterial compliance in normotensive and hypertensive rats independently of its effects on the arterial blood pressure. (Hypertension 1991;17:534-540)

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Section: Discussionmentioning

confidence: 99%

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confidence: 99%

Effects of alpha 1-blockade on arterial compliance in normotensive and hypertensive rats.

1991

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“…The pharmacological studies demonstrated a positive inotropic effect of saterinone, which is at least partially due to PDE inhibition and partially due to a vasodilation caused mainly by ␣ 1 -adrenoceptor antagonism (2,7). Another possible mechanism responsible for vasodilation might be central 5-HT 1A receptor stimulation as it has been described for urapidil (20).…”

Section: Discussionmentioning

confidence: 90%

“…It should be mentioned that the hypotensive effect of urapidil is not only due to postsynaptic ␣ 1 -adrenoceptor blockade but also involves a central mechanism, possibly antagonism at the central 5-HT 1A receptors (20). To our knowledge, the possibility that saterinone may have a similar additional central mechanism of hypotensive action has not yet been explored.…”

Section: Pharmacologymentioning

confidence: 99%

Saterinone, a Phosphodiesterase (PDE) III Inhibitor and α₁‐Adrenergic Antagonist

Kieback

Baumann

1999

Cardiovascular Drug Reviews

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“…Urapidil is a new selective IX 1 -adrenorcceptor antagonist. Apart from its a 1 -adrenoreceptor•blocking potency, which is somewhat less selective than that of prazosin, urapidil may also affect vascular tone through central mechanisms involving stimulation of serotonin lA (5•HT 1 A) receptors [18].…”

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confidence: 99%

Effects of sodium-nitroprusside and urapidil on gas exchange and ventilation-perfusion relationships in patients with congestive heart failure

Adnot¹,

Radermacher²,

Andrivet³

et al. 1991

Eur Respir J

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Vasodilators usually decrease arterial PO2 in patients with congestive heart failure (CHF) because of alteration in ventilation-perfusion (Va/Q) relationships. The effects of sodium nitroprusside (SNP) and urapidil (U), a new selective alpha 1-receptor antagonist, were investigated in seven patients with CHF. The distribution of ventilation and perfusion was examined using the multiple gas elimination technique. The haemodynamic responses to SNP and U were similar, cardiac index increasing by 25% with SNP and by 31% with U. Despite a similar increase of mixed venous oxygen tension, the arterial PO2 decreased from 11.3 +/- 0.8 to 9.6 +/- 0.6 kPa (p less than 0.01) with SNP but remained unchanged (11.0 +/- 0.9 vs 11.4 +/- 0.8 kPa, NS) with U. SNP and U both increased perfusion to lung units with Va/Q ratios of 0.1 or less with no change in shunt fraction. The fractional perfusion to total low Va/Q ratios (low Va/Q + shunt) was higher with SNP than with U (14.1 +/- 2.6 vs 9.5 +/- 2.3%, p less than 0.01). The results suggest that gas exchange and Va/Q relationships are altered less with U than with SNP in patients with CHF.

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Pharmacologic profile of urapidil

Cited by 19 publications

References 25 publications

Effects of alpha 1-blockade on arterial compliance in normotensive and hypertensive rats.

Effects of alpha 1-blockade on arterial compliance in normotensive and hypertensive rats.

Saterinone, a Phosphodiesterase (PDE) III Inhibitor and α₁‐Adrenergic Antagonist

Effects of sodium-nitroprusside and urapidil on gas exchange and ventilation-perfusion relationships in patients with congestive heart failure

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Pharmacologic profile of urapidil

Cited by 19 publications

References 25 publications

Effects of alpha 1-blockade on arterial compliance in normotensive and hypertensive rats.

Effects of alpha 1-blockade on arterial compliance in normotensive and hypertensive rats.

Saterinone, a Phosphodiesterase (PDE) III Inhibitor and α1‐Adrenergic Antagonist

Effects of sodium-nitroprusside and urapidil on gas exchange and ventilation-perfusion relationships in patients with congestive heart failure

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Product

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Saterinone, a Phosphodiesterase (PDE) III Inhibitor and α₁‐Adrenergic Antagonist