PMID: 8584609Oct 1, 1995Paper

Tolerability, safety and pharmacokinetics of single dose and multiple dosing of the selective D1 antagonist NNC 01-0687 in healthy subjects

Psychopharmacology
B K SkrumsagerM Seiberling

Abstract

Selective dopamine D1-receptor antagonists have been shown to exhibit similar effects in animal models for antipsychotic action as the selective D2 antagonists. NNC 01-0687, a benzazepine with selective and high affinity to the D1-receptor, was well tolerated by healthy subjects allocated to double blind, placebo controlled studies. Complaints of moderate restlessness and drowsiness were reported after administration of 25 mg NNC 01-0687, indicating the dose to be the maximum tolerated single dose. The highest multiple dose level of a daily dose of 45 mg NNC 01-0687 administered t.i.d. for 14 days was assessed as safe and well-tolerated with few reports of adverse events. Some alanine aminotransferase (ALT) elevations appeared in both treatment groups (active and placebo) and no evident influence of NNC 01-0687 on the liver function could be derived. No statistically significant or clinically relevant effects were observed in haematological parameters, urinalyses, blood pressure, heart rate, ECG or plasma levels of prolactin, cortisol or growth hormone. The plasma drug concentration curves indicated a fast absorption with tmax at 0.5-1 h and an apparent elimination half-life of 3-4 h. Both AUC and Cmax appeared to be linearly c...Continue Reading

References

Mar 1, 1992·Neurochemistry International·V L CoffinA Barnett
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Jan 1, 1990·Behavioural Pharmacology·B.A. Ellenbroek, A.R. Cools

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Citations

Oct 1, 1995·Psychopharmacology·T R Barnes, J Gerlach
May 27, 2003·Journal of Psychiatric Research·Derek N EderGordon Wildschiødtz
Nov 1, 1996·European Journal of Pediatrics·W L RobsonA K Leung
Jan 3, 2007·Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics·Barbara BennettNathalie Toublanc
Sep 5, 2012·ChemMedChem·Antonio NardiAchim Kless

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