Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus

Neuropharmacology. 1994 Jan;33(1):61-6. doi: 10.1016/0028-3908(94)90097-3.

Abstract

The selective 5-hydroxytryptamine1A (5-HT1A) agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT, 0.5-35 micrograms kg-1 i.v.) produces a dose related reversible inhibition (ED50 = 6.5 micrograms kg-1 i.v.) of the firing of serotonergic neurones in the dorsal raphe nucleus of the guinea-pig. Administration of N-tert-butyl-3- (4-(2-methoxyphenyl)piperazine-1-yl)-2phenylpropanamide dihydrochloride (WAY100135, 0.5 mg kg-1 i.v.), a specific 5-HT1A antagonist, antagonized the 8-OHDPAT induced inhibition of neuronal firing whilst methyl 4-(4-[4-(1,1,3-trioxo-2H-1,2-benzoisothiazol-2-yl)butyl]-1- piperazinyl) 1 H-indole-2-carboxylate (SDZ 216-525, 0.1-0.5 mg kg-1 i.v.) (also a putative 5-HT1A antagonist) reduced the basal firing of 5-HT neurones and furthermore failed to antagonize the inhibition produced by 8-OHDPAT. These results indicate that WAY 100135 is a silent and selective 5-HT1A antagonist whereas SDZ 216-525 demonstrates a partial agonist activity at the somatodendritic 5-HT1A autoreceptor in the guinea-pig DRN.

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin / antagonists & inhibitors
  • 8-Hydroxy-2-(di-n-propylamino)tetralin / pharmacology
  • Animals
  • Dose-Response Relationship, Drug
  • Guinea Pigs
  • In Vitro Techniques
  • Indoles / pharmacology*
  • Male
  • Neurons / drug effects*
  • Piperazines / pharmacology*
  • Raphe Nuclei / cytology
  • Raphe Nuclei / drug effects*
  • Serotonin / physiology*
  • Serotonin Antagonists*
  • Serotonin Receptor Agonists / pharmacology
  • Thiazoles / pharmacology*

Substances

  • Indoles
  • Piperazines
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • Thiazoles
  • WAY 100135
  • SDZ 216-525
  • Serotonin
  • 8-Hydroxy-2-(di-n-propylamino)tetralin