SB-216641A

Modify Date: 2025-08-25 16:35:24

SB-216641A Structure
SB-216641A structure
Common Name SB-216641A
CAS Number 193611-67-5 Molecular Weight 523.02300
Density N/A Boiling Point N/A
Molecular Formula C28H31ClN4O4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of SB-216641A


SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A blocks SKF-99101H from functioning in vivo[1][2].

 Names

Name N-{3-[2-(Dimethylamino)ethoxy]-4-methoxyphenyl}-2'-methyl-4'-(5-m ethyl-1,2,4-oxadiazol-3-yl)-4-biphenylcarboxamide hydrochloride ( 1:1)

 SB-216641A Biological Activity

Description SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A blocks SKF-99101H from functioning in vivo[1][2].
Related Catalog
Target

5-HT1B Receptor

5-HT1D Receptor

In Vivo SB-216641A (0.6–20 mg/kg;腹腔注射;单剂量) 在豚鼠内以剂量依赖性方式阻碍 SKF-99101H 诱导的低体温[1]。 SB-216641A (559 nmol/kg;静脉注射;单剂量) 与 5-HT1B/D 受体拮抗剂 GR-127935 联用时改善了狗注射 800 nmol/kg 舒马曲坦 Sumatriptan (HY-B0121B) 后观察到的胃松弛[2]。 Animal Model: Guinea pigs[1]. Dosage: 0.6, 2.0, 6.0 and 20.0 mg/kg. Administration: Intraperitoneal injection; single dose. Result: Significantly blocked the effects of SKF-99101H. Animal Model: Dogs[2]. Dosage: 559 nmol/kg. Administration: Intravenous injection; single dose. Result: Improved the gastric relaxation.
References

[1]. Hagan JJ, et al. Stimulation of 5-HT1B receptors causes hypothermia in the guinea pig. Eur J Pharmacol. 1997 Jul 23;331(2-3):169-74.  

[2]. De Ponti F, et al. Role of 5-HT1B/D receptors in canine gastric accommodation: effect of sumatriptan and 5-HT1B/D receptor antagonists. Am J Physiol Gastrointest Liver Physiol. 2003 Jul;285(1):G96-104.  

 Chemical & Physical Properties

Molecular Formula C28H31ClN4O4
Molecular Weight 523.02300
Exact Mass 522.20300
PSA 89.72000
LogP 6.09670
InChIKey JPBMDMNORXKGHZ-UHFFFAOYSA-N
SMILES COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1OCCN(C)C.Cl
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