4-(5-isothiocyanato-1,2,3,4-tetrahydro-1-naphthyl)-1H-imidazole: An imidazole-type affinity label for the α1-adrenergic receptor

W. Zheng, L. Jing, P. N. Patil, L. Lei, D. R. Feller, Duane Miller

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Based on the conformationally restricted analog 5 of medetomidine (4), a prototypic compound of the novel imidazole class of (α2-adrenergic receptor (AR) agonists, compound 6 was prepared and evaluated at human platelet (α2-AR and rat aorta (α1-AR. Functional studies indicated that compound 6 behaves as an irreversible antagonist (affinity label) at (α1-AR, but a reversible antagonist at (α2-AR. Compound 6 may serve as a lead for developing new generation and possibly subtype-selective (α1-AR affinity labels.

Original languageEnglish (US)
Pages (from-to)318-327
Number of pages10
JournalMedicinal Chemistry Research
Volume10
Issue number5
StatePublished - Jan 1 2001

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Affinity Labels
Adrenergic Receptors
Medetomidine
Adrenergic Agonists
Platelets
Aorta
Rats
Blood Platelets
imidazole

All Science Journal Classification (ASJC) codes

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

Cite this

4-(5-isothiocyanato-1,2,3,4-tetrahydro-1-naphthyl)-1H-imidazole : An imidazole-type affinity label for the α1-adrenergic receptor. / Zheng, W.; Jing, L.; Patil, P. N.; Lei, L.; Feller, D. R.; Miller, Duane.

In: Medicinal Chemistry Research, Vol. 10, No. 5, 01.01.2001, p. 318-327.

Research output: Contribution to journalArticle

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