The regional localization of a new potent centrally acting antihypertensive agent R 28935 and its less active threo isomer R 29814 in the cat brain

A.J.M. Loonen; W. Soudijn; H.H. Van Rooy; I. Van Wijngaarden

doi:10.1016/0014-2999(77)90010-3

The regional localization of a new potent centrally acting antihypertensive agent R 28935 and its less active threo isomer R 29814 in the cat brain

A.J.M. Loonen, W. Soudijn, H.H. Van Rooy, I. Van Wijngaarden

Research output: Contribution to journal › Article › Academic › peer-review

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Abstract

Systemic administration of the centrally acting antihypertensive agent R 28935 to cats resulted in a long lasting decrease of mean arterial pressure (±30%) whereas the same dose of the threo-isomer R 29814 was ineffective. The antihypertensive activity was due to the unaltered drug. In spite of an identical log P, pKa, dose and a comparable plasma level, the concentration of R 28935 in all the brain areas tested was about twice that of the threo-isomer, suggesting a stereoselective uptake and/or binding of R 28935.

Original language	English
Pages (from-to)	281-285
Number of pages	5
Journal	European Journal of Pharmacology
Volume	45
Issue number	3
DOIs	https://doi.org/10.1016/0014-2999(77)90010-3
Publication status	Published - 22-Apr-1977
Externally published	Yes

Keywords

1 [1 [2 (1,4 benzodioxan 2 yl) 2 hydroxyethyl] 4 piperidyl] 2 benzimidazolinone
radioisotope
tritium
unclassified drug
blood pressure
brain
cat
drug absorption
drug binding
drug distribution
drug isomer
erythro 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3
pharmacokinetics
plasma
stereochemistry
theoretical study
threo 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3

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10.1016/0014-2999(77)90010-3

The regional localisation of a new potent centrally acting antihypertensive agent R 28935 and its less active threo-isomer R 29814 in the cat brainFinal publisher's version, 332 KBLicence: CC BY

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title = "The regional localization of a new potent centrally acting antihypertensive agent R 28935 and its less active threo isomer R 29814 in the cat brain",

abstract = "Systemic administration of the centrally acting antihypertensive agent R 28935 to cats resulted in a long lasting decrease of mean arterial pressure (±30%) whereas the same dose of the threo-isomer R 29814 was ineffective. The antihypertensive activity was due to the unaltered drug. In spite of an identical log P, pKa, dose and a comparable plasma level, the concentration of R 28935 in all the brain areas tested was about twice that of the threo-isomer, suggesting a stereoselective uptake and/or binding of R 28935.",

keywords = "1 [1 [2 (1,4 benzodioxan 2 yl) 2 hydroxyethyl] 4 piperidyl] 2 benzimidazolinone, radioisotope, tritium, unclassified drug, blood pressure, brain, cat, drug absorption, drug binding, drug distribution, drug isomer, erythro 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3, pharmacokinetics, plasma, stereochemistry, theoretical study, threo 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3",

author = "A.J.M. Loonen and W. Soudijn and {Van Rooy}, H.H. and {Van Wijngaarden}, I.",

year = "1977",

month = apr,

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doi = "10.1016/0014-2999(77)90010-3",

language = "English",

volume = "45",

pages = "281--285",

journal = "European Journal of Pharmacology",

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T1 - The regional localization of a new potent centrally acting antihypertensive agent R 28935 and its less active threo isomer R 29814 in the cat brain

AU - Loonen, A.J.M.

AU - Soudijn, W.

AU - Van Rooy, H.H.

AU - Van Wijngaarden, I.

PY - 1977/4/22

Y1 - 1977/4/22

N2 - Systemic administration of the centrally acting antihypertensive agent R 28935 to cats resulted in a long lasting decrease of mean arterial pressure (±30%) whereas the same dose of the threo-isomer R 29814 was ineffective. The antihypertensive activity was due to the unaltered drug. In spite of an identical log P, pKa, dose and a comparable plasma level, the concentration of R 28935 in all the brain areas tested was about twice that of the threo-isomer, suggesting a stereoselective uptake and/or binding of R 28935.

AB - Systemic administration of the centrally acting antihypertensive agent R 28935 to cats resulted in a long lasting decrease of mean arterial pressure (±30%) whereas the same dose of the threo-isomer R 29814 was ineffective. The antihypertensive activity was due to the unaltered drug. In spite of an identical log P, pKa, dose and a comparable plasma level, the concentration of R 28935 in all the brain areas tested was about twice that of the threo-isomer, suggesting a stereoselective uptake and/or binding of R 28935.

KW - 1 [1 [2 (1,4 benzodioxan 2 yl) 2 hydroxyethyl] 4 piperidyl] 2 benzimidazolinone

KW - radioisotope

KW - tritium

KW - unclassified drug

KW - blood pressure

KW - brain

KW - cat

KW - drug absorption

KW - drug binding

KW - drug distribution

KW - drug isomer

KW - erythro 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3

KW - pharmacokinetics

KW - plasma

KW - stereochemistry

KW - theoretical study

KW - threo 1 {1 [2 (2,3 dihydro 1,4 benzodioxin 2 yl) 2 hydroxyethyl] 4 piperidinyl} 1,3 dihydro 2h benzimidazol 2 one h 3

U2 - 10.1016/0014-2999(77)90010-3

DO - 10.1016/0014-2999(77)90010-3

M3 - Article

SN - 0014-2999

VL - 45

SP - 281

EP - 285

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

IS - 3

ER -

The regional localization of a new potent centrally acting antihypertensive agent R 28935 and its less active threo isomer R 29814 in the cat brain

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Keywords

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