Zolantidine dimaleate

Names

[ Name ]:
Zolantidine dimaleate

[Synonym ]:
2-Benzothiazolamine, N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]-, (2Z)-2-butenedioate (1:2)
AL1YII70LM
Zolantidine dimaleate
N-{3-[3-(Piperidin-1-ylmethyl)phenoxy]propyl}-1,3-benzothiazol-2-amine (2Z)-but-2-enedioate (1:2)
N-[3-[3-(1-Piperidinylmethyl)phenoxy]propyl]-2-benzothiazolamine dimaleate
SKF 95282 dimaleate
SKF-95282 dimaleate salt
N-{3-[3-(1-Piperidinylmethyl)phenoxy]propyl}-1,3-benzothiazol-2-amine (2Z)-2-butenedioate (1:2)

Biological Activity

[Description]:

Zolantidine dimaleate (SKF 95282 dimaleate) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine dimaleate induces antinociception[1][2].

[Related Catalog]:

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

[Target]

H2 Receptor

[In Vivo]

Zolantidine dimaleate (5、10、20、40 mg/kg；皮下注射) 在胆汁淤积大鼠中诱导抗伤害作用[2]。 Animal Model: 200-250 g, male Wistar rats (cholestatic rats)[2] Dosage: 5, 10, 20, 40 mg/kg Administration: S.c. Result: Significantly increased tail-flick latencies and induced antinociception.

[References]

[1]. Calcutt CR, et al. Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist. Br J Pharmacol. 1988 Jan;93(1):69-78.

[2]. Hasanein P. Two histamine H2 receptor antagonists, zolantidine and cimetidine, modulate nociception in cholestatic rats. J Psychopharmacol. 2011 Feb;25(2):281-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₀H₃₅N₃O₉S

[ Molecular Weight ]:
613.68

[ Exact Mass ]:
613.209412

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist.

Br. J. Pharmacol. 93(1) , 69-78, (1988)

1. The novel benzthiazole derivative zolantidine (SK&F 95282) is a potent antagonist of histamine at H2-receptors in guinea-pig atrium and rat uterus. Only apparent pA2 values of 7.46 and 7.26 respect...

Linking solubility and permeability assays for maximum throughput and reproducibility.

J. Biomol. Screen. 10(4) , 383-90, (2005)

Solubility and permeability are intimately linked in drug absorption processes. They have, however, been traditionally assayed separately. To support this linkage, a combined solubility/permeability a...

Identification of novel functional inhibitors of acid sphingomyelinase.

PLoS ONE 6 , e23852, (2011)

We describe a hitherto unknown feature for 27 small drug-like molecules, namely functional inhibition of acid sphingomyelinase (ASM). These entities named FIASMAs (Functional Inhibitors of Acid Sphing...