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Chemical Compound Review

MOLI000120     N-[[(2S)-1-ethylpyrrolidin-2- yl]methyl]-5...

Synonyms: AC1L9NGH
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Disease relevance of Epidepride


Psychiatry related information on Epidepride


High impact information on Epidepride


Chemical compound and disease context of Epidepride


Anatomical context of Epidepride

  • Scatchard analysis of epidepride binding to alpha 2 noradrenergic receptors in the frontal cortex and hippocampus revealed an apparent KD of 9 nM [7].
  • Correlation of inhibition of [3H]spiperone and [125I]epidepride binding to striatal membranes by a variety of D2 ligands revealed a correlation coefficient of 0.99, indicating that epidepride labels a D2 site [7].

Associations of Epidepride with other chemical compounds


Gene context of Epidepride

  • Both direct and indirect binding studies with [125I]epidepride and unlabeled epidepride, respectively, demonstrated that the affinity of D-2 receptors for the ligand was decreased from 20 to 30 pM in the presence of sodium to 350 to 500 pM in the absence of sodium [11].
  • [123I] Epidepride binding was significantly reduced in both striata of dystonia patients compared with controls (p < 0.05) [8].
  • Epidepride [(S)-(-)-N-([1-ethyl-2-pyrrolidinyl]methyl)-5-iodo-2,3-dimethoxybenza mide] binds with a picomolar affinity (Ki = 24 pM) to the dopamine D2 receptor [9].
  • Epidepride, (S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodo-2,3-dimethoxybenzamide+ ++, the iodine analogue of isoremoxipride (FLB 457), was found to be a very potent dopamine D2 receptor antagonist [7].

Analytical, diagnostic and therapeutic context of Epidepride

  • [(125)I]Epidepride, which binds with high affinity to DA D(2) and D(3) receptors, was used in autoradiographic studies to determine the distribution and density of D(2)-like receptors, and the epidepride analogue [(18)F]fallypride positron was used for positron emission tomography studies to delineate D(2)-like receptors in vivo [12].


  1. Regulation and functional characterization of a rat recombinant dopamine D3 receptor. Cox, B.A., Rosser, M.P., Kozlowski, M.R., Duwe, K.M., Neve, R.L., Neve, K.A. Synapse (1995) [Pubmed]
  2. Alterations in locomotor activity after microinjections of GBR-12909, selective dopamine antagonists or neurotensin into the medial prefrontal cortex. Radcliffe, R.A., Erwin, V.G. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  3. Clinical deficits in Huntington disease correlate with reduced striatal uptake on iodine-123 epidepride single-photon emission tomography. Leslie, W.D., Greenberg, C.R., Abrams, D.N., Hobson, D. European journal of nuclear medicine. (1999) [Pubmed]
  4. Absolute quantitation of iodine-123 epidepride kinetics using single-photon emission tomography: comparison with carbon-11 epidepride and positron emission tomography. Almeida, P., Ribeiro, M.J., Bottlaender, M., Loc'h, C., Langer, O., Strul, D., Hugonnard, P., Grangeat, P., Mazière, B., Bendriem, B. European journal of nuclear medicine. (1999) [Pubmed]
  5. Mapping the genes for haloperidol-induced catalepsy. Kanes, S., Dains, K., Cipp, L., Gatley, J., Hitzemann, B., Rasmussen, E., Sanderson, S., Silverman, M., Hitzemann, R. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  6. Characterization of dopamine transporter and locomotor effects of cocaine, GBR 12909, epidepride, and SCH 23390 in C57BL and DBA mice. Womer, D.E., Jones, B.C., Erwin, V.G. Pharmacol. Biochem. Behav. (1994) [Pubmed]
  7. High affinity dopamine D2 receptor radioligands. 2. [125I]epidepride, a potent and specific radioligand for the characterization of striatal and extrastriatal dopamine D2 receptors. Kessler, R.M., Ansari, M.S., Schmidt, D.E., de Paulis, T., Clanton, J.A., Innis, R., al-Tikriti, M., Manning, R.G., Gillespie, D. Life Sci. (1991) [Pubmed]
  8. Imaging the pre- and postsynaptic side of striatal dopaminergic synapses in idiopathic cervical dystonia: a SPECT study using [123I] epidepride and [123I] beta-CIT. Naumann, M., Pirker, W., Reiners, K., Lange, K.W., Becker, G., Brücke, T. Mov. Disord. (1998) [Pubmed]
  9. Carbon-11 epidepride: a suitable radioligand for PET investigation of striatal and extrastriatal dopamine D2 receptors. Langer, O., Halldin, C., Dollé, F., Swahn, C.G., Olsson, H., Karlsson, P., Hall, H., Sandell, J., Lundkvist, C., Vaufrey, F., Loc'h, C., Crouzel, C., Mazière, B., Farde, L. Nucl. Med. Biol. (1999) [Pubmed]
  10. Pharmacokinetics of the three radioiodinated dopamine D2 receptor ligands [123I]IBF, [123I]epidepride and [123I]2'-ISP in nonhuman primates. Baldwin, R.M., Zea-Ponce, Y., Zoghbi, S.S., al-Tikriti, M.S., Seibyl, J.P., Sybirska, E.H., Malison, R.T., Laruelle, M., Charney, D.S., Hoffer, P.B. Nucl. Med. Biol. (1994) [Pubmed]
  11. Sodium-dependent isomerization of dopamine D-2 receptors characterized using [125I]epidepride, a high-affinity substituted benzamide ligand. Neve, K.A., Henningsen, R.A., Kinzie, J.M., De Paulis, T., Schmidt, D.E., Kessler, R.M., Janowsky, A. J. Pharmacol. Exp. Ther. (1990) [Pubmed]
  12. Distribution of dopamine D2-like receptors in the human thalamus: autoradiographic and PET studies. Rieck, R.W., Ansari, M.S., Whetsell, W.O., Deutch, A.Y., Kessler, R.M. Neuropsychopharmacology (2004) [Pubmed]
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