Battle of Honey Springs

PNU-142633 is an experimental drug candidate for the treatment of migraine. It exerts its effect as a selective, high affinity 5-HT1D receptor antagonist.[1][2] PNU-142633 is well tolerated after oral administration.[3]

It was an interesting candidate due to its greater affinity for 5-HT1D compared to 5-HT1B receptors (typical migraine drugs such as triptans are agonists for both receptors), but experimental results were disappointing.[4]

The structure can be compared favorably with Sonepiprazole.

References

  1. ^ Pregenzer, JF; Alberts, GL; Im, WB; Slightom, JL; Ennis, MD; Hoffman, RL; Ghazal, NB; Tenbrink, RE (1999). "Differential pharmacology between the guinea-pig and the gorilla 5-HT1D receptor as probed with isochromans (5-HT1D-selective ligands)". British Journal of Pharmacology. 127 (2): 468–72. doi:10.1038/sj.bjp.0702532. PMC 1566017. PMID 10385247.
  2. ^ PNU 142633, Santa Cruz Biotechnology
  3. ^ Fleishaker, JC; Pearson, LK; Knuth, DW; Gomez-Mancilla, B; Francom, SF; McIntosh, MJ; Freestone, S; Azie, NE (1999). "Pharmacokinetics and tolerability of a novel 5-HT1D agonist, PNU-142633F". International Journal of Clinical Pharmacology and Therapeutics. 37 (10): 487–92. PMID 10543315.
  4. ^ The serotonin system : history, neuropharmacology, and pathology. M. D. Tricklebank, Eileen Daly. London, United Kingdom. 2019. ISBN 978-0-12-813324-8. OCLC 1105199268.{{cite book}}: CS1 maint: location missing publisher (link) CS1 maint: others (link)


source: https://en.wikipedia.org/wiki/PNU-142633