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Chemical Compound Review

CHEMBL543760     5,6-dimethoxy-N,N-dipropyl- 2,3-dihydro-1H...

Synonyms: PNU-99194A, CID119195, DCL001028, AR-1G6208, LS-173451, ...
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Disease relevance of Tocris-1357

  • By itself, U 99194A failed to significantly alter the emesis produced by any of the cited agonists, however, it potentiated (3-8 times) the antiemetic effects of sulpride both in reducing the number of shrews vomiting as well as decreasing the mean vomiting frequency with the following ID50 order: PD 128, 907 < 7-(OH) DPAT < quinpirole [1].

Psychiatry related information on Tocris-1357

  • Against scopolamine-induced amnesia, SB-277011 (24 mg/kg p.o.) was equally potent in showing protective efficacy; however, two times higher dose levels of U-99194A (24 mg/kg s.c.) and RGH-1756 (2 mg/kg p.o.) were required to attenuate the scopolamine-induced impairment [2].
  • Finally, to assess the role of D3 receptor actions in the stimulus generalization produced by (+)-7-OH-DPAT (0.1 mg/kg), PNU-99194A (10, 20 mg/kg) was tested in combination with this compound in each training group [3].
  • In habituated rats it had no significant effect on motor activity and was not able to antagonize the hypoactivity caused by PD 128907 (0.1 mg/kg s.c.). U 99194A (5, 10 and 20 mg/kg s.c.) dose-dependently and significantly increased motor activity in mice and inhibited the effects of both agonists [4].
  • Pretreatment with the dopamine D3 antagonist U 99194 eliminated the disturbance of passive avoidance learning induced by 7-OH-DPAT [5].

High impact information on Tocris-1357

  • Treatment of mice with a D3 antagonist U-99194A selectively reduced homing of naive CD8+ T cells into lymph nodes [6].
  • PNU-99194A, a D3 receptor-preferring antagonist, induced a CPP itself at the dose of 10 mg/kg but not at 5 or 15 mg/kg and impaired significantly at 10 and 15 mg/kg the morphine-induced CPP [7].
  • Preferential dopamine D(3) antagonists, cis-(+)-(1S, 2R)-5-methoxy-1-methyl-2-(di-n-propylamino)tetralin HCl [(+)-UH232] and 5,6-dimethoxy-2-(di-n-propylamine)indan (U-99194A) resulted in a greater increase in the evoked dopamine released from the nucleus accumbens compared with that from the striatum [8].
  • Aim of present study was to investigate in male Wistar rats, whether behavioral response to hot plate test application could be influenced by systemic administration of 7-OH-DPAT, a dopaminergic (DA) D3 versus D2 receptor agonist, or U 99194, a DA D3 versus D2 receptor antagonist [9].
  • None of the doses of SB-277011 (5, 20 mg/kg), the most selective dopamine D3 antagonist to date, and the lower dose (12 mg/kg) of the moderately D3 selective antagonist U-99194A could influence the rate of self-administration [10].

Chemical compound and disease context of Tocris-1357


Biological context of Tocris-1357

  • Pretreatment with pramipexole in a concentration range (4-100 microM) significantly attenuates DA- or L-DOPA-induced cytotoxicity and apoptosis, an action which is not blocked by D3 antagonist U-99194 A or D2 antagonist raclopride [12].

Anatomical context of Tocris-1357

  • It is suggested that D3 receptors in transfected CHO cells may exert mainly an inhibitory, but also a stimulatory influence on TPA-induced AA release, and that PNU-99194A acts as an agonist in this system [13].

Analytical, diagnostic and therapeutic context of Tocris-1357


  1. The role of D2 and D3 dopamine receptors in the mediation of emesis in Cryptotis parva (the least shrew). Darmani, N.A., Zhao, W., Ahmad, B. Journal of neural transmission (Vienna, Austria : 1996) (1999) [Pubmed]
  2. Dopamine D3 receptor antagonists improve the learning performance in memory-impaired rats. Laszy, J., Laszlovszky, I., Gyertyán, I. Psychopharmacology (Berl.) (2005) [Pubmed]
  3. The dopamine D3 receptor antagonist PNU-99194A fails to block (+)-7-OH-DPAT substitution for D-amphetamine or cocaine. Baker, L.E., Svensson, K.A., Garner, K.J., Goodwin, A.K. Eur. J. Pharmacol. (1998) [Pubmed]
  4. 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]
  5. The effects of selective dopamine agonists on a passive avoidance learning task in the day-old chick. Hale, M.W., Crowe, S.F. Behavioural pharmacology. (2002) [Pubmed]
  6. Dopamine selectively induces migration and homing of naive CD8+ T cells via dopamine receptor D3. Watanabe, Y., Nakayama, T., Nagakubo, D., Hieshima, K., Jin, Z., Katou, F., Hashimoto, K., Yoshie, O. J. Immunol. (2006) [Pubmed]
  7. Dopamine D3 receptor ligands modulate the acquisition of morphine-conditioned place preference. Francès, H., Smirnova, M., Leriche, L., Sokoloff, P. Psychopharmacology (Berl.) (2004) [Pubmed]
  8. Dopamine D(3) receptors modulate evoked dopamine release from slices of rat nucleus accumbens via muscarinic receptors, but not from the striatum. Yamada, S., Harano, M., Annoh, N., Tanaka, M. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  9. Effects of 7-OH-DPAT and U 99194 on the behavioral response to hot plate test, in rats. Casarrubea, M., Sorbera, F., Crescimanno, G. Physiol. Behav. (2006) [Pubmed]
  10. Targeting the dopamine D3 receptor cannot influence continuous reinforcement cocaine self-administration in rats. Gál, K., Gyertyán, I. Brain Res. Bull. (2003) [Pubmed]
  11. Analysis of D2 and D3 receptor-selective ligands in rats trained to discriminate cocaine from saline. Garner, K.J., Baker, L.E. Pharmacol. Biochem. Behav. (1999) [Pubmed]
  12. Neuroprotection by pramipexole against dopamine- and levodopa-induced cytotoxicity. Zou, L., Jankovic, J., Rowe, D.B., Xie, W., Appel, S.H., Le, W. Life Sci. (1999) [Pubmed]
  13. Both dopamine and the putative dopamine D3 receptor antagonist PNU-99194A induce a biphasic inhibition of phorbol ester-stimulated arachidonic acid release from CHO cells transfected with the dopamine D3 receptor. Nilsson, C.L., Hellstrand, M., Ekman, A., Eriksson, E. Life Sci. (1999) [Pubmed]
  14. 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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