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147116-67-4

147116-67-4 structure
147116-67-4 structure
  • Name: Maropitant
  • Chemical Name: (2S,3S)-2-benzhydryl-N-[(5-tert-butyl-2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
  • CAS Number: 147116-67-4
  • Molecular Formula: C32H40N2O
  • Molecular Weight: 468.67300
  • Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
  • Create Date: 2016-06-22 07:44:28
  • Modify Date: 2024-01-10 13:51:22
  • Maropitant is a neurokinin (NK1) receptor antagonist. IC50 value:Target: NK1 receptorMaropitant is the first NK1 receptor antagonist developed to treat and prevent emesis in dogs. Treatment with 1 mg/kg Maropitant citrate, significantly reduced the size of ulcerative dermatitis (UD) lesions in mice. Intravenous Maropitant decreased (p < 0.05) MAC by 16% (1.74 ± 0.17%). In contrast, epidural administration of either saline or Maropitant did not change (p > 0.05) the MAC (2.17 ± 0.34% and 1.92 ± 0.12%, respectively).

Name (2S,3S)-2-benzhydryl-N-[(5-tert-butyl-2-methoxyphenyl)methyl]-1-azabicyclo[2.2.2]octan-3-amine
Synonyms 4XE2T9H4DH
UNII-4XE2T9H4DH
Maropitant
Maropitant Citrate Salt
CS-1065
Description Maropitant is a neurokinin (NK1) receptor antagonist. IC50 value:Target: NK1 receptorMaropitant is the first NK1 receptor antagonist developed to treat and prevent emesis in dogs. Treatment with 1 mg/kg Maropitant citrate, significantly reduced the size of ulcerative dermatitis (UD) lesions in mice. Intravenous Maropitant decreased (p < 0.05) MAC by 16% (1.74 ± 0.17%). In contrast, epidural administration of either saline or Maropitant did not change (p > 0.05) the MAC (2.17 ± 0.34% and 1.92 ± 0.12%, respectively).
Related Catalog
References

[1]. Hay Kraus BL. Efficacy of maropitant in preventing vomiting in dogs premedicated with hydromorphone. Vet Anaesth Analg. 2013 Jan;40(1):28-34.

[2]. Lesman SP, Boucher JF, Grover GS, et al. The pharmacokinetics of maropitant citrate dosed orally to dogs at 2 mg/kg and 8 mg/kg once daily for 14 days consecutive days. J Vet Pharmacol Ther. 2012 Nov 20.

[3]. Alvillar BM, Boscan P, Mama KR, et al. Effect of epidural and intravenous use of the neurokinin-1 (NK-1) receptor antagonist maropitant on the sevoflurane minimum alveolar concentration (MAC) in dogs. Vet Anaesth Analg. 2012 Mar;39(2):201-5.

[4]. Ramsey DS, Kincaid K, Watkins JA et al. Safety and efficacy of injectable and oral maropitant, a selective neurokinin 1 receptor antagonist, in a randomized clinical trial for treatment of vomiting in dogs. J Vet Pharmacol Ther. 2008 Dec;31(6):538-43. doi: 10.1111/j.1365-2885.2008.00992.x.

[5]. Benchaoui HA, Cox SR, Schneider RP et al. The pharmacokinetics of maropitant, a novel neurokinin type-1 receptor antagonist, in dogs. J Vet Pharmacol Ther. 2007 Aug;30(4):336-44.

[6]. Maropitant

Molecular Formula C32H40N2O
Molecular Weight 468.67300
Exact Mass 468.31400
PSA 24.50000
LogP 6.70600
Storage condition 2-8℃

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147116-67-4 structure

147116-67-4

Literature: WO2005/75473 A1, ; Page/Page column 16; 21-22 ;
Precursor  1

DownStream  1