Literature DB >> 6689366

Synthesis and some pharmacological properties of a conformationally restricted imipramine analogue.

C J Grol, G Westenberg, B Hazelhoff, J De Vries.   

Abstract

The synthesis of the semi-rigid imipramine analogue 2-(N,N-dimethylaminomethylene)-2,3,7,8-tetrahydro-1H-quino[1,8-ab] [I]-benzazepine is described. The compound was pharmacologically evaluated in a number of general in vivo screening tests for antidepressive activity. From these preliminary tests the compound appeared to show an imipramine-like activity. However, it did not have an effect on the noradrenaline depletion by 4, alpha-dimethyl-m-tyramine. These results are discussed on the basis of the conformational requirements determining the pharmacological profile of antidepressants.

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Year:  1983        PMID： 6689366     DOI： 10.1007/bf02074864

Source DB:  PubMed          Journal:  Pharm Weekbl Sci        ISSN： 0167-6555


  10 in total

1.  Possible pharmacological and theoretical implications of x-ray structure of the tricyclic antidepressant imipramine.

Authors:  M L Post; O Kennard; A S Horn
Journal:  Nature       Date:  1974-12-06       Impact factor: 49.962

2.  Effects of some antidepressant drugs on the depletion of intraneuronal brain catecholamine stores caused by 4,alpha-dimethyl-meta-tyramine.

Authors:  A Carlsson; H Corrodi; K Fuxe; T Hökfelt
Journal:  Eur J Pharmacol       Date:  1969-03       Impact factor: 4.432

3.  Catecholamine uptake by synaptosomes from rat brain. Structure-activity relationships of drugs with differential effects on dopamine and norepinephrine neurons.

Authors:  A S Horn; J T Coyle; S H Snyder
Journal:  Mol Pharmacol       Date:  1971-01       Impact factor: 4.436

4.  Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.

Authors:  A R Martin; V M Paradkar; G W Peng; R C Speth; H I Yamamura; A S Horn
Journal:  J Med Chem       Date:  1980-08       Impact factor: 7.446

5.  Effects of drugs on the disposition of H-3-norepinephrine in the rat brain.

Authors:  J Glowinski; J Axelrod
Journal:  Pharmacol Rev       Date:  1966-03       Impact factor: 25.468

6.  Synthesis and pharmacological evaluation of conformationally restricted phenothiazine analogues.

Authors:  C J Grol; D Dijkstra; W Schunselaar; B H Westerink; A R Martin
Journal:  J Med Chem       Date:  1982-01       Impact factor: 7.446

7.  Selective inhibition of noradrenaline and serotonin uptake by C 49802-B-Ba and CGP 6085 A.

Authors:  P C Waldmeier; P A Baumann; M Wilhelm; R Bernasconi; L Maître
Journal:  Eur J Pharmacol       Date:  1977-12-15       Impact factor: 4.432

8.  Pharmacological evaluation of 2-(4-methylaminobutoxy)diphenylmethane hydrochloride (MCI-2016), a new psychotropic drug with antidepressant activity.

Authors:  A Tobe; Y Yoshida; H Ikoma; S Tonomura; R Kikumoto
Journal:  Arzneimittelforschung       Date:  1981

9.  Effects of antidepressant drugs on different receptors in the brain.

Authors:  H Hall; S O Ogren
Journal:  Eur J Pharmacol       Date:  1981-03-26       Impact factor: 4.432

10.  THE INCREASE IN THE TOXICITY OF YOHIMBINE INDUCED BY IMIPRAMINE AND OTHER DRUGS IN MICE.

Authors:  R M QUINTON
Journal:  Br J Pharmacol Chemother       Date:  1963-08
  10 in total

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