PMID: 22454938Dec 1, 1974

The effects of oral AH 5158, a combined α and β-adrenoceptor antagonist, in healthy volunteers

British Journal of Clinical Pharmacology
D A RichardsJ G Maconochie


1 In healthy male volunteers after single oral doses, AH 5158 produced inhibition of exercise induced tachycardia, falls in systolic and diastolic pressure at rest and in response to exercise, which are probably related to combined β- and α-adrenoceptor antagonism. 2 At increasing doses from 100 mg to 400 mg there exists a dose related antagonistic effect, though the dominant effect of β-adrenoceptor antagonism is more easily demonstrable than is α antagonism. 3 As indicated by the pattern of pharmacological effects, absorption of the oral drug is good and the duration of action of a 400 mg dose is approximately 8 hours. 4 Despite being administered in β-adrenoceptor blocking doses, AH 5158 had no adverse effects upon peak expiratory flow at rest or in response to exercise. 5 It is concluded that the pharmacological profile of this combined α- and β-adrenoceptor antagonism suggests a potential therapeutic role as an antihypertensive drug.


May 6, 1972·Lancet·L Beilin, B E Juel-Jensen
Feb 1, 1972·British Journal of Pharmacology·J G CollierB F Robinson
Aug 1, 1972·British Journal of Pharmacology·J B FarmerR J Marshall
Aug 1, 1974·British Journal of Clinical Pharmacology·G M BerlyneC Yoran


Jan 3, 1977·European Journal of Clinical Pharmacology·D A RichardsL E Martin
Jan 1, 1978·General Pharmacology·A G Blakeley, R J Summers
Jan 1, 1981·General Pharmacology·D E Potter, J M Rowland
Oct 1, 1976·British Journal of Clinical Pharmacology·D A RichardsB N Prichard
Feb 1, 1977·British Journal of Clinical Pharmacology·D A RichardsJ G Maconochie
Apr 1, 1977·British Journal of Clinical Pharmacology·J G MaconochieD A Richards
Sep 1, 1979·Postgraduate Medical Journal·M A Frais, T J Bayley
Jan 1, 1980·Current Medical Research and Opinion·J TuomilehtoJ Elo
Aug 1, 1984·British Journal of Clinical Pharmacology·D P NichollsR G Shanks
Dec 1, 1985·British Journal of Clinical Pharmacology·P C O'ConnorR G Shanks
Jun 1, 1980·British Journal of Clinical Pharmacology·O ThulesiusE Berlin
Sep 1, 1981·British Journal of Clinical Pharmacology·A J Riley, E J Riley
Aug 1, 1976·Australian and New Zealand Journal of Medicine·E A RoseiP M Trust
Oct 1, 1979·Scottish Medical Journal·D G Lambie
Jun 1, 1982·British Journal of Clinical Pharmacology·T TakedaR Shigiya
Apr 5, 1980·The Medical Journal of Australia·I MacdonaldP Kincaid-Smith
Apr 1, 1979·British Journal of Clinical Pharmacology·B N Prichard, D A Richards

Related Concepts

Antihypertensive Agents
Human Volunteers
Hydrocarbons, Aromatic
Alpha-adrenergic receptor
Beta-adrenergic receptor
Oral Cavity
Diastolic Blood Pressure

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.

Adrenergic Receptors: Trafficking

Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here.