Cannabaceae

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PNU-142633
Names
Preferred IUPAC name
(1S)-1-{2-[4-(4-Carbamoylphenyl)piperazin-1-yl]ethyl}-N-methyl-3,4-dihydro-1H-2-benzopyran-6-carboxamide
Other names
PNU-142633F
Identifiers
3D model (JSmol)
ChemSpider
UNII
  • InChI=1S/C24H30N4O3/c1-26-24(30)19-4-7-21-18(16-19)9-15-31-22(21)8-10-27-11-13-28(14-12-27)20-5-2-17(3-6-20)23(25)29/h2-7,16,22H,8-15H2,1H3,(H2,25,29)(H,26,30)/t22-/m0/s1
    Key: PNTVCCRNJOGKGA-QFIPXVFZSA-N
  • InChI=1/C24H30N4O3/c1-26-24(30)19-4-7-21-18(16-19)9-15-31-22(21)8-10-27-11-13-28(14-12-27)20-5-2-17(3-6-20)23(25)29/h2-7,16,22H,8-15H2,1H3,(H2,25,29)(H,26,30)/t22-/m0/s1
    Key: PNTVCCRNJOGKGA-QFIPXVFZBB
  • NC(C(C=C1)=CC=C1N2CCN(CC[C@@H]3OCCC4=C3C=CC(C(NC)=O)=C4)CC2)=O
Properties
C24H30N4O3
Molar mass 422.529 g·mol−1
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).

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

[edit]
  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

One thought on “Cannabaceae”

  1. Well, that’s interesting to know that Psilotum nudum are known as whisk ferns. Psilotum nudum is the commoner species of the two. While the P. flaccidum is a rare species and is found in the tropical islands. Both the species are usually epiphytic in habit and grow upon tree ferns. These species may also be terrestrial and grow in humus or in the crevices of the rocks.
    View the detailed Guide of Psilotum nudum: Detailed Study Of Psilotum Nudum (Whisk Fern), Classification, Anatomy, Reproduction

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