The polymorphism of the CNS active compound Org 13011 was studied using different crystallisation methods (i.e. different solvents and cooling rates). The samples were analysed by Raman, solid state NMR, X-ray powder diffraction (XRPD) and thermal analysis. This led to the characterisation of two crystalline forms A and B. Further high temperature analysis using Raman, XRPD, solid state NMR and DSC revealed another two (high temperature) crystalline forms C and D. The transitions to the high temperature crystalline forms occur at temperatures of about 60 degrees C. This study shows that the application of high temperature experiments is useful and can lead to the discovery of new crystalline forms.

01 Jun 1999·European NeuropsychopharmacologyQ3 · MEDICINE

Antagonism of the 5-HT1A receptor stimulus in a conditioned taste aversion procedure

Q3 · MEDICINE

Article

Author: Berendsen, Hemmie H. G. ; Broekkamp, Chris L. E.

The conditioned taste aversion procedure in mice was used to test for blockade of the drug stimulus of the 5-HT1A receptor agonists (+/-)-8-hydroxy-2-(di-n-propylamino)tetralin HBr (8-OH-DPAT), 1-(4-trifluoromethyl-2-pyridinyl)-4- [4-[2-oxo-1-pyrrolidinyl]butyl]piperazine (E)-2-butenedioate (Org 13011) and the 5-HT reuptake inhibitor fluoxetine. The conditioned taste aversion induced by 8-OH-DPAT (0.22 mg/kg) and Org 13011 (0.5 mg/kg) was readily blocked by the 5-HT1A receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexanecarboxamide trihydrochloride (WAY-100635) (0.1 mg/kg). The conditioned taste aversion induced by fluoxetine could not be antagonized by WAY-100635 nor by the 5-HT2 receptor antagonist mianserin. It is concluded that the conditioned taste aversion induced by 8-OH-DPAT or Org 13011 is mediated via 5-HT1A receptors. The results suggest that the conditioned taste aversion induced by fluoxetine is not exclusively mediated by 5-HT1A receptors nor exclusively by 5-HT2 receptors. The results also indicate that the conditioned taste aversion paradigm can be used to test for antagonism of stimulus properties of compounds.

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Indication	Highest Phase	Country/Location	Organization	Date
Depressive Disorder	Phase 2	-	Merck Sharp & Dohme Corp.	-

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