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Chemical Compound Review

Anpirtolina     2-chloro-6-(4- piperidylsulfanyl)pyridine

Synonyms: Anpirtoline, Anpirtolinum, Tocris-0703, CHEMBL1316374, BPBio1_001089, ...
 
 
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Psychiatry related information on Anpirtoline

  • 6. In the electrostimulated pain test using mice, anpirtoline dose-dependently increased the pain threshold with an ED50 of 0.52 mg kg-1, i.p. The antinociceptive activity of anpirtoline was abolished by pretreatment with cyproheptadine or propranolol.(ABSTRACT TRUNCATED AT 250 WORDS)[1]
  • The effective inhibition of high levels of aggressive behavior due to alcohol consumption after anpirtoline treatment confirm the 5-HT1B receptor as a critical site in the termination of aggression [2].
  • Coadministration of the selective 5HT1A agonist 8-OH-DPAT (0.03-1.25 mg/kg S.C.) with anpirtoline (2.5 mg/kg) induced a dramatic increase in locomotor activity and a behavioural syndrome identical to that produced by RU24969 [3].
 

High impact information on Anpirtoline

  • The ability of the 5-HT1B receptor agonist anpirtoline and the selective 5-HT1B receptor antagonist NAS-181 to affect spatial learning in the water maze (WM) and aversive learning in the passive avoidance (PA) task were examined in the rat [4].
  • Aggression escalated by social instigation or by discontinuation of reinforcement ("frustration") in mice: inhibition by anpirtoline: a 5-HT1B receptor agonist [5].
  • Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5-HT1A and 5-HT1B receptor agonists 8-OH-DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD-299 and NAS-181 [6].
  • In this respect, anpirtoline mimicked other 5-HT3 receptor antagonists; the rank order of potency was ondansetron > anpirtoline > metoclopramide [7].
  • Whereas 5-HT was equipotent in both tissues (EC50 = 69 nM), anpirtoline was markedly less potent in pig brain cortex slices (EC50 = 1190 nM) than in rat brain cortex slices (EC50 = 55 nM) [1].
 

Anatomical context of Anpirtoline

  • 2. In radioligand binding studies on rat brain cortical membranes, anpirtoline inhibited specific binding of [3H]-(S)-zacopride to 5-HT3 receptor recognition sites (pKi: 7.53) [7].
  • In the chronic anpirtoline experiment, 5-HT synthesis rates of almost all of the projection areas, as well as the raphe nuclei, were normalized or had a tendency to be normalized [8].
 

Associations of Anpirtoline with other chemical compounds

  • 4. In superfused rat and pig brain cortex slices preincubated with [3H]-5-HT, the electrically evoked tritium overflow was inhibited by anpirtoline and 5-HT [1].
  • [3] This also applies to the 5-HT1B receptor agonist and antagonist anpirtoline (0.3-4.0 micromol kg(-1)) and isamoltane (1.0-64.0 micromol kg(-1)), respectively [9].
 

Gene context of Anpirtoline

 

Analytical, diagnostic and therapeutic context of Anpirtoline

References

  1. Anpirtoline, a novel, highly potent 5-HT1B receptor agonist with antinociceptive/antidepressant-like actions in rodents. Schlicker, E., Werner, U., Hamon, M., Gozlan, H., Nickel, B., Szelenyi, I., Göthert, M. Br. J. Pharmacol. (1992) [Pubmed]
  2. Oral drug self-administration in the home cage of mice: alcohol-heightened aggression and inhibition by the 5-HT1B agonist anpirtoline. Miczek, K.A., de Almeida, R.M. Psychopharmacology (Berl.) (2001) [Pubmed]
  3. RU24969-induced behavioural syndrome requires activation of both 5HT1A and 5HT1B receptors. O'Neill, M.F., Parameswaran, T. Psychopharmacology (Berl.) (1997) [Pubmed]
  4. Analysis of the role of the 5-HT1B receptor in spatial and aversive learning in the rat. Ahlander-Lüttgen, M., Madjid, N., Schött, P.A., Sandin, J., Ogren, S.O. Neuropsychopharmacology (2003) [Pubmed]
  5. Aggression escalated by social instigation or by discontinuation of reinforcement ("frustration") in mice: inhibition by anpirtoline: a 5-HT1B receptor agonist. de Almeida, R.M., Miczek, K.A. Neuropsychopharmacology (2002) [Pubmed]
  6. Facilitation and inhibition of male rat ejaculatory behaviour by the respective 5-HT1A and 5-HT1B receptor agonists 8-OH-DPAT and anpirtoline, as evidenced by use of the corresponding new and selective receptor antagonists NAD-299 and NAS-181. Hillegaart, V., Ahlenius, S. Br. J. Pharmacol. (1998) [Pubmed]
  7. 5-HT3 receptor antagonism by anpirtoline, a mixed 5-HT1 receptor agonist/5-HT3 receptor antagonist. Göthert, M., Hamon, M., Barann, M., Bönisch, H., Gozlan, H., Laguzzi, R., Metzenauer, P., Nickel, B., Szelenyi, I. Br. J. Pharmacol. (1995) [Pubmed]
  8. Effects of anpirtoline on regional serotonin synthesis in the rat brain: an autoradiographic study. Watanabe, A., Nakai, A., Tohyama, Y., Nguyen, K.Q., Diksic, M. Nucl. Med. Biol. (2006) [Pubmed]
  9. Non-serotonergic potentiation by (-)-pindolol of DOI-induced forward locomotion in rats: possible involvement of beta-adrenoceptors?. Kaur, P., Ahlenius, S. Journal of neural transmission (Vienna, Austria : 1996) (2000) [Pubmed]
  10. Pharmacological characterisation of the decrease in 5-HT synthesis in the mouse brain evoked by the selective serotonin re-uptake inhibitor citalopram. Stenfors, C., Yu, H., Ross, S.B. Naunyn Schmiedebergs Arch. Pharmacol. (2001) [Pubmed]
  11. The effects of selective serotonin-reuptake inhibitor on visual evoked potential in rats. Iwamura, Y., Fujii, Y., Kamei, C. J. Pharmacol. Sci. (2004) [Pubmed]
  12. Serotonin-1B receptor activity and expression modulate the aggression-stimulating effects of adolescent anabolic steroid exposure in hamsters. Grimes, J.M., Melloni, R.H. Behav. Neurosci. (2005) [Pubmed]
 
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