Azidomorphines and homopyrimidazols: a new approach to the ideal analgetic

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Azidomorphines, new semi-synthetic isomorphine alkaloids and homopyrimidazols (1.5-diazanaphtalenes), two new families of compounds favourably enlarging the scope of analgetics, were developed. Azidomorphine, a 40-50 times more potent analgetic in man than morphine, showed a remarkably great dissociation between analgetic potency and dependence capacity and proved to exert significantly fewer unfavourable effects than either morphine or pentazocine. Probon (Rymazolium), the first compound of the homopyrimidazol series, introduced to therapy as a new minor analgetic, potentiated the analgetic and antagonized the respiratory depressant effect of morphine and its derivatives. In patients with chronic intractable pain, a combination of azidomorphine (0.5 mg) and Probon (150 mg) achieved total pain relief without noticeable euphoria and none of the patients subjected to nalorphine-precipitation showed signs of abstinence according to the Himmelsbach scoring system. Since both the azidomorphines and the homopyrimidazols are unexploited new families, further progress in detailed structure-activity relationship studies seems quite promising.

Original languageEnglish
Pages (from-to)3-11
Number of pages9
JournalActa Physiologica et Pharmacologica Bulgarica
Volume3
Issue number2
Publication statusPublished - 1977

Fingerprint

Morphine
Morphine Derivatives
Nalorphine
Pentazocine
Intractable Pain
Structure-Activity Relationship
Alkaloids
Chronic Pain
Pain
homopyrimidazoles
probon
azidomorphine
Therapeutics

ASJC Scopus subject areas

  • Physiology
  • Pharmacology

Cite this

Azidomorphines and homopyrimidazols : a new approach to the ideal analgetic. / Knoll, J.

In: Acta Physiologica et Pharmacologica Bulgarica, Vol. 3, No. 2, 1977, p. 3-11.

Research output: Contribution to journalArticle

@article{2829b2d7591c4a49b7d813bd8e179f46,
title = "Azidomorphines and homopyrimidazols: a new approach to the ideal analgetic",
abstract = "Azidomorphines, new semi-synthetic isomorphine alkaloids and homopyrimidazols (1.5-diazanaphtalenes), two new families of compounds favourably enlarging the scope of analgetics, were developed. Azidomorphine, a 40-50 times more potent analgetic in man than morphine, showed a remarkably great dissociation between analgetic potency and dependence capacity and proved to exert significantly fewer unfavourable effects than either morphine or pentazocine. Probon (Rymazolium), the first compound of the homopyrimidazol series, introduced to therapy as a new minor analgetic, potentiated the analgetic and antagonized the respiratory depressant effect of morphine and its derivatives. In patients with chronic intractable pain, a combination of azidomorphine (0.5 mg) and Probon (150 mg) achieved total pain relief without noticeable euphoria and none of the patients subjected to nalorphine-precipitation showed signs of abstinence according to the Himmelsbach scoring system. Since both the azidomorphines and the homopyrimidazols are unexploited new families, further progress in detailed structure-activity relationship studies seems quite promising.",
author = "J. Knoll",
year = "1977",
language = "English",
volume = "3",
pages = "3--11",
journal = "Acta Physiologica et Pharmacologica Bulgarica",
issn = "0323-9950",
publisher = "Universitetsko Izdatelstvo Sv. Kliment Okhridski/Publishing House of the Sofia University St. Kilment Ohridski",
number = "2",

}

TY - JOUR

T1 - Azidomorphines and homopyrimidazols

T2 - a new approach to the ideal analgetic

AU - Knoll, J.

PY - 1977

Y1 - 1977

N2 - Azidomorphines, new semi-synthetic isomorphine alkaloids and homopyrimidazols (1.5-diazanaphtalenes), two new families of compounds favourably enlarging the scope of analgetics, were developed. Azidomorphine, a 40-50 times more potent analgetic in man than morphine, showed a remarkably great dissociation between analgetic potency and dependence capacity and proved to exert significantly fewer unfavourable effects than either morphine or pentazocine. Probon (Rymazolium), the first compound of the homopyrimidazol series, introduced to therapy as a new minor analgetic, potentiated the analgetic and antagonized the respiratory depressant effect of morphine and its derivatives. In patients with chronic intractable pain, a combination of azidomorphine (0.5 mg) and Probon (150 mg) achieved total pain relief without noticeable euphoria and none of the patients subjected to nalorphine-precipitation showed signs of abstinence according to the Himmelsbach scoring system. Since both the azidomorphines and the homopyrimidazols are unexploited new families, further progress in detailed structure-activity relationship studies seems quite promising.

AB - Azidomorphines, new semi-synthetic isomorphine alkaloids and homopyrimidazols (1.5-diazanaphtalenes), two new families of compounds favourably enlarging the scope of analgetics, were developed. Azidomorphine, a 40-50 times more potent analgetic in man than morphine, showed a remarkably great dissociation between analgetic potency and dependence capacity and proved to exert significantly fewer unfavourable effects than either morphine or pentazocine. Probon (Rymazolium), the first compound of the homopyrimidazol series, introduced to therapy as a new minor analgetic, potentiated the analgetic and antagonized the respiratory depressant effect of morphine and its derivatives. In patients with chronic intractable pain, a combination of azidomorphine (0.5 mg) and Probon (150 mg) achieved total pain relief without noticeable euphoria and none of the patients subjected to nalorphine-precipitation showed signs of abstinence according to the Himmelsbach scoring system. Since both the azidomorphines and the homopyrimidazols are unexploited new families, further progress in detailed structure-activity relationship studies seems quite promising.

UR - http://www.scopus.com/inward/record.url?scp=0017566472&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0017566472&partnerID=8YFLogxK

M3 - Article

C2 - 74199

AN - SCOPUS:0017566472

VL - 3

SP - 3

EP - 11

JO - Acta Physiologica et Pharmacologica Bulgarica

JF - Acta Physiologica et Pharmacologica Bulgarica

SN - 0323-9950

IS - 2

ER -