Molecular aspects of the receptor activation by imidazolines

An overview

P. N. Patil, D. R. Feller, Duane Miller

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

Based on the pharmacological activity of chiral imidazolines the steric requirements for the activation of the α-adrenoceptor are provided. Importantly, the sequence of interaction of the critical groups of the asymmetric carbon of imidazolines and catecholamines with the α-adrenoceptor is postulated. Thus, initial determinants of molecular efficacy are hypothesized. The effect of aromatic fluoro-substitution and introduction of a double bond in the imidazoline moiety on the pharmacologic activity is discussed. The unique mechanism of non-adrenergic vascular activity of isothiocyanato-tolazoline is presented.

Original languageEnglish (US)
Pages (from-to)187-194
Number of pages8
JournalJournal of Neural Transmission, Supplement
Issue number34
StatePublished - Dec 1 1991

Fingerprint

Imidazoline Receptors
Imidazolines
Adrenergic Receptors
Tolazoline
Catecholamines
Blood Vessels
Carbon
Pharmacology

All Science Journal Classification (ASJC) codes

  • Neurology
  • Clinical Neurology
  • Psychiatry and Mental health
  • Biological Psychiatry

Cite this

Molecular aspects of the receptor activation by imidazolines : An overview. / Patil, P. N.; Feller, D. R.; Miller, Duane.

In: Journal of Neural Transmission, Supplement, No. 34, 01.12.1991, p. 187-194.

Research output: Contribution to journalArticle

@article{1c506c82c9ab4496b1fa2afaab1b7ac2,
title = "Molecular aspects of the receptor activation by imidazolines: An overview",
abstract = "Based on the pharmacological activity of chiral imidazolines the steric requirements for the activation of the α-adrenoceptor are provided. Importantly, the sequence of interaction of the critical groups of the asymmetric carbon of imidazolines and catecholamines with the α-adrenoceptor is postulated. Thus, initial determinants of molecular efficacy are hypothesized. The effect of aromatic fluoro-substitution and introduction of a double bond in the imidazoline moiety on the pharmacologic activity is discussed. The unique mechanism of non-adrenergic vascular activity of isothiocyanato-tolazoline is presented.",
author = "Patil, {P. N.} and Feller, {D. R.} and Duane Miller",
year = "1991",
month = "12",
day = "1",
language = "English (US)",
pages = "187--194",
journal = "Journal of Neural Transmission, Supplement",
issn = "0303-6995",
publisher = "Springer Wien",
number = "34",

}

TY - JOUR

T1 - Molecular aspects of the receptor activation by imidazolines

T2 - An overview

AU - Patil, P. N.

AU - Feller, D. R.

AU - Miller, Duane

PY - 1991/12/1

Y1 - 1991/12/1

N2 - Based on the pharmacological activity of chiral imidazolines the steric requirements for the activation of the α-adrenoceptor are provided. Importantly, the sequence of interaction of the critical groups of the asymmetric carbon of imidazolines and catecholamines with the α-adrenoceptor is postulated. Thus, initial determinants of molecular efficacy are hypothesized. The effect of aromatic fluoro-substitution and introduction of a double bond in the imidazoline moiety on the pharmacologic activity is discussed. The unique mechanism of non-adrenergic vascular activity of isothiocyanato-tolazoline is presented.

AB - Based on the pharmacological activity of chiral imidazolines the steric requirements for the activation of the α-adrenoceptor are provided. Importantly, the sequence of interaction of the critical groups of the asymmetric carbon of imidazolines and catecholamines with the α-adrenoceptor is postulated. Thus, initial determinants of molecular efficacy are hypothesized. The effect of aromatic fluoro-substitution and introduction of a double bond in the imidazoline moiety on the pharmacologic activity is discussed. The unique mechanism of non-adrenergic vascular activity of isothiocyanato-tolazoline is presented.

UR - http://www.scopus.com/inward/record.url?scp=0026357976&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0026357976&partnerID=8YFLogxK

M3 - Article

SP - 187

EP - 194

JO - Journal of Neural Transmission, Supplement

JF - Journal of Neural Transmission, Supplement

SN - 0303-6995

IS - 34

ER -