Antihypertensive Agents 1962–1968

Schier, O.; Marxer, A.

doi:10.1007/978-3-0348-7068-9_2

Cited by 7 publications

(9 citation statements)

References 179 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…BW A575C, at these doses, had no effect on resting blood pressure and heart rate of the conscious dog. At both dose levels, dose-ratios obtained demonstrated that BW A575C was twice as potent as an ACE inhibitor than as a P-adrenoceptor blocking agent ( There is an extensive body of knowledge delineating structure-activity relationships of both P-adrenoceptor blocking agents and ACE inhibitors (Schier & Marker, 1981;Patchett & Cordes, 1985). Both classes of agents have broad overlapping structural requirements for activity, each being able to accept a range of aromatic systems to provide highly active compounds.…”

Section: Introductionmentioning

confidence: 99%

BW A575C, a chemically novel agent with angiotensin converting enzyme inhibitor and β‐adrenoceptor‐blocking properties

Allan

Cambridge

Hardy

et al. 1987

British J Pharmacology

View full text Add to dashboard Cite

) is a chemically novel agent which exhibits in a single molecule both angiotensin converting enzyme (ACE) inhibition and P-adrenoceptor-blocking properties.2 BW A575C produced a competitive blockade of heart rate responses to isoprenaline in a guinea-pig right atrial preparation (pKB 7.18 ± 0.05, cf. pindolol 8.9 ± 0.7). BW A575C inhibited a partially purified preparation of ACE obtained from rabbit lung (IC50 10.7 + 2.1 nM, cf. enalaprilat, 4.4 ± 0.8 nM).3 Intravenous administration of BW A575C (1-100 tgkg-' min-')to the pithed rat inhibited in a dose-dependent fashion both angiotensin I-induced pressor responses and isoprenaline-induced tachycardia. Dose-ratios obtained from such studies demonstrated that, in this preparation, BW A575C was approximately 100 times more active as an ACE inhibitor than as a P-adrenoceptor blocking agent. 4 Intravenous administration of BW A575C (I mg kg-') to the conscious rat inhibited angiotensin Iinduced pressor responses, being approximately equipotent to enalapril and 10 times more potent than captopril. At the same dose, BW A575C had a similar duration of action as an ACE inhibitor to enalapril. 5 Intravenous administration of BW A575C (I mg kg-') to either conscious dogs or rats inhibited both angiotensin I-induced pressor responses and isoprenaline-induced heart rate responses. Doseratios obtained from such studies demonstrated that in these species, BW A575C was 2-10 times more active as an ACE inhibitor than as a P-adrenoceptor blocking agent.

show abstract

Section: Introductionmentioning

confidence: 99%

BW A575C, a chemically novel agent with angiotensin converting enzyme inhibitor and β‐adrenoceptor‐blocking properties

Allan

Cambridge

Hardy

et al. 1987

British J Pharmacology

View full text Add to dashboard Cite

show abstract

“…Soc. see also SCHIER and MARXER (1969), CARSTENS (1972), andDE STEVENS, WILHELM (1976). LEROY (1909) stated "no remedy can or will reduce the blood pressure so kindly and so quickly, when given after a proper manner than the thiocyanates".…”

Section: E Schlittlermentioning

confidence: 95%

“…The most recent review of SCHIER and MARXER (1969) does not report on hydralazine and its analogs. However, this lead has been actively followed up and in the patent literature a series of new results have been published.…”

Section: Compounds Acting Directly On Vascular Smooth Muscles A)mentioning

confidence: 96%

See 1 more Smart Citation

The Chemistry of Antihypertensive Agents

Schlittler¹

1977

Antihypertensive Agents

View full text Add to dashboard Cite

“…Antihypertensive 'side effects' were observed in 1941 by MAE [222], while evaluating aminoquinolines as potential antimalarials. The consequent pursuit of this clue by various research laboratories [223] led to a series of 2-amino-6,7-dimethoxy-quinazolines that were assessed as potential antihypertensives by Pfizer [224]. 2-Piperazino-4-amino-6,7-dimethoxy-quinazoline, prazosin (CXIII), showed antihypertensive efficacy of therapeutic significance and was introduced as a peripheral vasodilator in 1974.…”

Section: Prazosinmentioning

confidence: 99%