Hexahydrobenzo[a]phenanthridines

novel dopamine D3 receptor ligands

Val J. Watts, Cindy P. Lawler, Timm Knoerzer, Mechelle A. Mayleben, Kim A. Neve, David E. Nichols, Richard Mailman

Research output: Contribution to journalArticle

31 Citations (Scopus)

Abstract

We report that certain substituted hexathydrobenzo[a]phenanthridines are novel high affinity ligands selective for the dopamine D3 receptor. These data demonstrate that substitutions on the heterocyclic nitrogen and the pendant phenyl ring of this nucleus cause a marked increase in both affinity and selectivity for dopamine D3 vs. D2 receptors. Thus, these compounds represent important new tools to study the pharmacology of dopamine D3 receptors, and may also provide an opportunity for the synthesis of new radioligands for dopamine D3 receptors.

Original languageEnglish (US)
Pages (from-to)271-273
Number of pages3
JournalEuropean Journal of Pharmacology
Volume239
Issue number1-3
DOIs
StatePublished - Aug 3 1993

Fingerprint

Phenanthridines
Dopamine D3 Receptors
Ligands
Dopamine
Nitrogen
Pharmacology

All Science Journal Classification (ASJC) codes

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Watts, V. J., Lawler, C. P., Knoerzer, T., Mayleben, M. A., Neve, K. A., Nichols, D. E., & Mailman, R. (1993). Hexahydrobenzo[a]phenanthridines: novel dopamine D3 receptor ligands. European Journal of Pharmacology, 239(1-3), 271-273. https://doi.org/10.1016/0014-2999(93)91012-C
Watts, Val J. ; Lawler, Cindy P. ; Knoerzer, Timm ; Mayleben, Mechelle A. ; Neve, Kim A. ; Nichols, David E. ; Mailman, Richard. / Hexahydrobenzo[a]phenanthridines : novel dopamine D3 receptor ligands. In: European Journal of Pharmacology. 1993 ; Vol. 239, No. 1-3. pp. 271-273.
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Watts, VJ, Lawler, CP, Knoerzer, T, Mayleben, MA, Neve, KA, Nichols, DE & Mailman, R 1993, 'Hexahydrobenzo[a]phenanthridines: novel dopamine D3 receptor ligands', European Journal of Pharmacology, vol. 239, no. 1-3, pp. 271-273. https://doi.org/10.1016/0014-2999(93)91012-C

Hexahydrobenzo[a]phenanthridines : novel dopamine D3 receptor ligands. / Watts, Val J.; Lawler, Cindy P.; Knoerzer, Timm; Mayleben, Mechelle A.; Neve, Kim A.; Nichols, David E.; Mailman, Richard.

In: European Journal of Pharmacology, Vol. 239, No. 1-3, 03.08.1993, p. 271-273.

Research output: Contribution to journalArticle

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T1 - Hexahydrobenzo[a]phenanthridines

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AU - Watts, Val J.

AU - Lawler, Cindy P.

AU - Knoerzer, Timm

AU - Mayleben, Mechelle A.

AU - Neve, Kim A.

AU - Nichols, David E.

AU - Mailman, Richard

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AB - We report that certain substituted hexathydrobenzo[a]phenanthridines are novel high affinity ligands selective for the dopamine D3 receptor. These data demonstrate that substitutions on the heterocyclic nitrogen and the pendant phenyl ring of this nucleus cause a marked increase in both affinity and selectivity for dopamine D3 vs. D2 receptors. Thus, these compounds represent important new tools to study the pharmacology of dopamine D3 receptors, and may also provide an opportunity for the synthesis of new radioligands for dopamine D3 receptors.

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Watts VJ, Lawler CP, Knoerzer T, Mayleben MA, Neve KA, Nichols DE et al. Hexahydrobenzo[a]phenanthridines: novel dopamine D3 receptor ligands. European Journal of Pharmacology. 1993 Aug 3;239(1-3):271-273. https://doi.org/10.1016/0014-2999(93)91012-C