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Digitale Medien

Benzylidenaminooxy-CarbonsÄure-Derivate als Auslöser von „Wet Dog Shake“-Verhalten bei normalen Ratten (1976)

Jahn, Ulrich ; Mixich, Georg

Springer

Psychopharmacology 46 (1976), S. 191-196

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ISSN: 1432-2072

Schlagwort(e): Chemically induced wet shake behavior ; Rats ; Benzylideneaminooxycarbonic acids ; Sgd 8473 ; Drug dependence ; Psychopharmacology ; Quasi-abstinence ; Methods

Quelle: Springer Online Journal Archives 1860-2000

Thema: Medizin

Notizen: Abstract Wet dog shake (WDS) behavior in rats, well known as morphine-withdrawal syndrome, could be elicited without concomitant symptoms for the first time chemically in nonmorphine-addicted animals. The capability to produce WDS was correlated with a specific chemical structure among the title-compounds. The threshold-dose of the most effective agents was 25–50 mg/kg, rather independent of the mode of application. Maximal responses of 10–20 WDS per min and animal were reached after application of 100–200 mg/kg. WDS behavior appeared within the first minutes after dose and lasted up to several hours. Detailed information is given on WDS-action of the substance Sgd 8473=α-[(4-chlorobenzylideneamino)-oxy]-isobutyric acid and the influence by different pharmacologic agents thereon. Inhibition of WDS was produced by: narcotic analgesics, narcotic antagonists, psychosedativ drugs, yohimbine, dl-amphetamine, cocaine, apomorphine and clonidine. Without influence on WDS were: physostigmine, atropine, ganglionic- or adrenergic-blocking drugs, Dopa, MAO-inhibitors, serotonin- and histamin-antagonists and nonnarcotic analgesics. To some extent chemically induced WDS seemed to be susceptible like precipitated WDS. So Sgd 8473 could be qualified for differentiating narcotic and nonnarcotic analgesics, for a “quasi-abstinence” agent in research of dependence mechanisms and for a tool in neuroanatomical studies of the CNS.

Materialart: Digitale Medien

URL: http://dx.doi.org/10.1007/BF00421391

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Digitale Medien

Nucleoside, 391) Angular und linear erweiterte Allopurinole:Pyrazolo[4,3-f]- und Pyrazolo[4,3-g] chinazolinone (1981)

Cuny, Eckehard ; Lichtenthaler, Frieder W. ; Jahn, Ulrich

Weinheim : Wiley-Blackwell

Berichte der deutschen chemischen Gesellschaft 114 (1981), S. 1624-1635

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ISSN: 0009-2940

Schlagwort(e): Chemistry ; Inorganic Chemistry

Quelle: Wiley InterScience Backfile Collection 1832-2000

Thema: Chemie und Pharmazie

Beschreibung / Inhaltsverzeichnis: Nucleosides, 391) Angular and Linear Extended Allopurinols: Pyrazolo[4,3-f]- and Pyrazolo[4,3-g]quinazolinonesFacile synthese have been developed for 3,8-dihydro-9H-pyrazolo[4,3-f]quinazolin-9-one (3), an angled benzolog of allopurinol (1a), and for the linear benzologously extended pyrazolo[4,3-g]-quinazolin-5-ones 4, 29, 30, and 31, involving five-step sequences starting with 5-aminoindazol (6) and 5-methyl-6-nitroindazol (17), respectively. 4 and 30 display a xanthine oxidase inhibition comparable to that of allopurinol, 4 also acting as a substrate, whereby it is oxidized to the 7-oxo derivative 31.

Notizen: Ausgehend von 5-Aminoindazol (6)bzw. 5-Methyl-6-nitroindazol (17) wurden einfache, jeweils fünfstufige Synthesen entwickelt für 3,8-Dihydro-9H-pyrazolo[4,3-f]chinazolin-9-on (3), einem gewinkelten Benzologen von Allopurinol (1a), und für die Pyrazolo [4,3-g]chinazolin-5-one 4, 29, 30 und 31, die gestreckt erweiterte Benzologe darstellen. 4 und 30 weisen eine dem Allopurinol vergleichbare Hemmung der Xanthin-Oxidase auf, wobei 4 unter Oxidation zum 7-Ox-Derivat 31 auch als Substrat fungiert.

Zusätzliches Material: 1 Ill.