Integrative cardiovascular actions of a novel catecholamine, GP-2-128

G. Abou-Mohamed, Robert William Caldwell, T. M. Ibrahim, R. R. Tuttle

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Systematic modification in the chemical structure of dobutamine resulted in production of a long-acting, highly potent catecholamine, GP-2-128 [(1- (3,4-dihydroxyphenyl)-2-[3-(4-carbamyl phenyl)-1-methyl-propylamino] ethanol)]. The cardiovascular actions of GP-2-128 were compared with those of isoproterenol (ISO) and dobutamine (DOB) in anesthetized dogs. GP-2-128 significantly increased left ventricular pressure (LVdP/dt(max)), cardiac output (CO), and heart rate (HR). It also reduced total peripheral vascular resistance (TPVR). For a given increase in contractility, changes in HR were greater after ISO than after GP-2-128 administration. DOB did not change HR significantly. Both GP-2-128 and DOB reduced TPVR, but ISO was more effective than GP-2-128 and DOB in reducing TPVR. GP-2-128 was 18,000 and 52 times more potent than DOB and ISO, respectively, in increasing LVdP/dt(max). For a given increase in contractility, the cardiovascular actions of GP-2-128 lasted significantly longer than those of DOB or ISO. A 50% mixture of the RR and RS distereoisomer forms of GP-2-128 (GP-2-114) have the same pharmacologic profile as the pure RR distereoisomer. Both GP-2-128 and GP-2- 114 produced current-dependent cardiovascular actions when administered by transdermal iontophoresis. The inotropic and chronotropic effects of GP-2- 128 are both largely due to stimulation of β-adrenoceptors, as shown by receptor blockade with propranolol. GP-2-128 is a very potent, long-acting catecholamine that can be administered by other than intravenous (i.v.) route.

Original languageEnglish (US)
Pages (from-to)485-491
Number of pages7
JournalJournal of Cardiovascular Pharmacology
Volume23
Issue number3
DOIs
StatePublished - Jan 1 1994

Fingerprint

Catecholamines
Dobutamine
Vascular Resistance
Isoproterenol
Heart Rate
1-(3,4-dihydroxyphenyl)-2-(3-(4-carbamylphenyl)-1-methylpropylamino)ethanol
Iontophoresis
Ventricular Pressure
Propranolol
Cardiac Output
Adrenergic Receptors
Ethanol
Dogs

Keywords

  • Cardiovascular
  • Dobutamine
  • Dogs
  • GP-2-128
  • Isoproterenol
  • Sympathomimetic amines

ASJC Scopus subject areas

  • Pharmacology
  • Cardiology and Cardiovascular Medicine

Cite this

Integrative cardiovascular actions of a novel catecholamine, GP-2-128. / Abou-Mohamed, G.; Caldwell, Robert William; Ibrahim, T. M.; Tuttle, R. R.

In: Journal of Cardiovascular Pharmacology, Vol. 23, No. 3, 01.01.1994, p. 485-491.

Research output: Contribution to journalArticle

Abou-Mohamed, G. ; Caldwell, Robert William ; Ibrahim, T. M. ; Tuttle, R. R. / Integrative cardiovascular actions of a novel catecholamine, GP-2-128. In: Journal of Cardiovascular Pharmacology. 1994 ; Vol. 23, No. 3. pp. 485-491.
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