Effect of a novel selective S1P1 agonist, Syl948, on mouse skin transplantation / 药学学报
Acta Pharmaceutica Sinica
; (12): 627-631, 2014.
Article
em Zh
| WPRIM
| ID: wpr-245036
Biblioteca responsável:
WPRO
ABSTRACT
Syl948 is a synthesized selective S1P1 agonist with novel structure. HTRF-IP1 test indicated that Syl948-P, the active form of Syl948 in vitro, has strong activity against S1P1 (EC50: 83 +/- 16 nmol x L(-1)), but its effect on S1P3 was very weak (EC50: 1 026 +/- 90 nmol x L(-1)). In SD rats, oral administration of Syl948 10 mg x kg(-1) significantly decreased the peripheral blood lymphocytes (PBL), with the maximal PBL inhibition rate of 63%, which was as similar as equal dose of fingolimod (FTY720). Oral administration of Syl948 10 mg x kg(-1) had no effect on heart rate of SD rats, which was better than FTY720. Daily oral administration with Syl948 (2 or 4 mg x kg(-1)) significantly prolonged the survival time of the allografts of skin slice on mice. In summary, the above results demonstrated that Syl948 has great selectivity in vitro and good activity in vivo, which indicated its potential use as an anti-rejection drug in skin transplantation.
Texto completo:
1
Base de dados:
WPRIM
Assunto principal:
Farmacologia
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Propilenoglicóis
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Esfingosina
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Transplante Homólogo
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Linfócitos
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Transplante de Pele
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Receptores de Lisoesfingolipídeo
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Cloridrato de Fingolimode
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Sobrevivência de Enxerto
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Imunossupressores
Limite:
Animals
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2014
Tipo de documento:
Article