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Chemical Compound Review

Nafadotride     N-[(1-butylpyrrolidin-2- yl)methyl]-4-cyano...

Synonyms: AC1MPBUT, CHEMBL286252, SureCN635866, CHEBI:64191, CHEBI:134432, ...
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Disease relevance of Nafadotride


Psychiatry related information on Nafadotride

  • In support of this view low doses of nafadotride, a novel D3 receptor-preferring antagonist, enhances locomotor activity in rodents, a behavioral response opposite to that of current neuroleptics [2].
  • The same nafadotride doses potentiated the grooming behavior induced by the D1 dopamine agonist SKF 38393 (10 mg/kg i.p.) as well as the stereotyped response to the D1/D2 agonist apomorphine (0.5 mg/kg s.c.). Stereotyped behavior was also observed in rats concomitantly treated with nafadotride and the D2 agonist quinpirole [3].

High impact information on Nafadotride

  • Adult, male, Sprague-Dawley rats were injected subcutaneously (s.c.) with the agonist 7-OH-DPAT (0.1 mg/kg) or antagonist nafadotride (1 mg/kg) at doses previously shown to produce negligible occupancy of D2 receptors in vivo [4].
  • Coperfusion with the D3 receptor-preferring antagonist nafadotride dose-dependently blocked the effect of 7-OH-DPAT on nucleus accumbens dopamine efflux [5].
  • In D(3) receptor knockout mice, MK-801-induced hyperactivity was weaker than that observed in wild-type mice while BP 897 and nafadotride were inactive [6].
  • Nafadotride, UH232 and AJ76, which show a mild preference for D3 versus D2 sites, blocked the PD128,907 DS, and the modestly-selective D3 antagonist, U99194A, was partially effective [7].
  • In vivo, all antagonists except GR 103,691 prevented the induction of hypothermia by (+)-PD 128,907 (0.63 mg/kg s.c.) and a further preferential D3 agonist, (+)-7-OH-DPAT (0.16 mg/kg s.c.). On the other hand, haloperidol, (+)-AJ 76, (+)-UH 232 and nafadotride all induced catalepsy in rats, whereas (+)-S 14297, U 99194 and GR 103,691 were inactive [8].

Chemical compound and disease context of Nafadotride

  • In mice habituated to the activity cage, nafadotride (0.1-3 mg/kg i.p.) caused a dose-dependent decrease in motor activity but did not affect the hypomotility evoked by either 7-OH-DPAT (0.1 mg/kg) or PD 128907 (0.1 mg/kg) [9].
  • In the present study, we compared the effects of dopamine D3 antagonists with different levels of selectivity over D2 receptors (nafadotride, U 99194A and SB 277011) on motor activity as well as on agonist-induced hypoactivity, in mice and rats [9].

Associations of Nafadotride with other chemical compounds


Gene context of Nafadotride

  • When administered alone, nafadotride did not change the expression of MOR mRNA [12].

Analytical, diagnostic and therapeutic context of Nafadotride


  1. Nafadotride, a potent preferential dopamine D3 receptor antagonist, activates locomotion in rodents. Sautel, F., Griffon, N., Sokoloff, P., Schwartz, J.C., Launay, C., Simon, P., Costentin, J., Schoenfelder, A., Garrido, F., Mann, A. J. Pharmacol. Exp. Ther. (1995) [Pubmed]
  2. The D3 receptor and its relevance in psychiatry. Schwartz, J.C., Griffon, N., Diaz, J., Levesque, D., Sautel, F., Sokoloff, P., Simon, P., Costentin, J., Garrido, F., Mann, A. International clinical psychopharmacology. (1995) [Pubmed]
  3. Nafadotride administration increases D1 and D1/D2 dopamine receptor mediated behaviors. Dall'Olio, R., Gaggi, R., Voltattorni, M., Tanda, O., Gandolfi, O. Behavioural pharmacology. (2002) [Pubmed]
  4. Increased levels of proneurotensin/neuromedin N mRNA in rat striatum and nucleus accumbens induced by 7-OH-DPAT and nafadotride. Levant, B., Garimelli, B., Shafer, R.A., Merchant, K.M. Neuropsychopharmacology (1999) [Pubmed]
  5. Neurochemical evidence that postsynaptic nucleus accumbens D3 receptor stimulation enhances cocaine reinforcement. Parsons, L.H., Caine, S.B., Sokoloff, P., Schwartz, J.C., Koob, G.F., Weiss, F. J. Neurochem. (1996) [Pubmed]
  6. The dopamine D3 receptor mediates locomotor hyperactivity induced by NMDA receptor blockade. Leriche, L., Schwartz, J.C., Sokoloff, P. Neuropharmacology (2003) [Pubmed]
  7. Discriminative stimulus properties of the dopamine D3 receptor agonists, PD128,907 and 7-OH-DPAT: a comparative characterization with novel ligands at D3 versus D2 receptors. Millan, M.J., Girardon, S., Monneyron, S., Dekeyne, A. Neuropharmacology (2000) [Pubmed]
  8. A comparative in vitro and in vivo pharmacological characterization of the novel dopamine D3 receptor antagonists (+)-S 14297, nafadotride, GR 103,691 and U 99194. Audinot, V., Newman-Tancredi, A., Gobert, A., Rivet, J.M., Brocco, M., Lejeune, F., Gluck, L., Desposte, I., Bervoets, K., Dekeyne, A., Millan, M.J. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  9. Effects of dopamine D3 receptor antagonists on spontaneous and agonist-reduced motor activity in NMRI mice and Wistar rats: comparative study with nafadotride, U 99194A and SB 277011. Gyertyán, I., Sághy, K. Behavioural pharmacology. (2004) [Pubmed]
  10. D3 receptor test in vitro predicts decreased cocaine self-administration in rats. Caine, S.B., Koob, G.F., Parsons, L.H., Everitt, B.J., Schwartz, J.C., Sokoloff, P. Neuroreport (1997) [Pubmed]
  11. Conversion of the modulatory actions of dopamine on spinal reflexes from depression to facilitation in D3 receptor knock-out mice. Clemens, S., Hochman, S. J. Neurosci. (2004) [Pubmed]
  12. Mu opioid receptor mRNA in nucleus accumbens is elevated following dopamine receptor activation. Azaryan, A.V., Clock, B.J., Cox, B.M. Neurochem. Res. (1996) [Pubmed]
  13. Anxiolytic-like effect of nafadotride and PNU 99194A, dopamine D3 receptor antagonists in animal models. Rogóz, Z., Kłodzińska, A., Maj, J. Polish journal of pharmacology. (2000) [Pubmed]
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