| Identification | Back Directory | [Name]
N-[2-(Dimethylamino)ethyl]-N-[[4′-[[(2-phenylethyl)amino]methyl][1,1′-biphenyl]-4-yl]methyl]-cyclopentanepropanamide dihydrochloride | [CAS]
864741-95-7 | [Synonyms]
SB 699551 dihydrochloride
3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[[4-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]propanamide | [Molecular Formula]
C34H46ClN3O | [MOL File]
864741-95-7.mol | [Molecular Weight]
548.21 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
H2O: soluble1mg/mL, clear (warmed) | [form ]
powder | [color ]
white to beige | [Water Solubility ]
H2O: 1mg/mL, clear (warmed) |
| Hazard Information | Back Directory | [Uses]
SB 699551 Dihydrochloride is a potent 5-HT5A receptor antagonist shown to mediate hypotension in anesthetized rats (1). May also be used as an antagonist in mediating the negative effects of schizophrenia. It is also used in the role of peripheral 5-HT5A receptors in 5-HT-induced cardiac sympatho-inhibition in type 1 diabetic rats. | [Biological Activity]
SB 699551 dihydrochloride is also known as (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4μ-{[(2-phenylethyl)amino]methyl}-4-biphenylyl)methyl]propanamide dihydrochloride). It is considered as a useful tool to explain the physiological roles of the 5-ht5A receptor.''SB-699551 is a 5-HT5A receptor antagonist(pKi = 8.3) with 100-fold selectivity over other 5-HT receptor populations. SB-699551 completely blocks 5-HT-induced [35S]GTPγS membrane binding in cells expressing recombinant guinea pig 5-HT-5A. | [in vivo]
SB-699551 (25 mg/kg; i.p.; once daily; 3 weeks) reduced xenograft growth rate in a breast cancer xenograft model in NOD/SCID mice and synergized with Docetaxel to reduce xenograft size[3].
SB-699551 (0.3-3 mg/kg; i.p.; once) reversed drug-induced cognitive deficits in attention switching and novel object recognition tasks and improved social withdrawal in Sprague-Dawley rats[7].
SB-699551 (0.3-3 mg/kg; s.c.; once) co-treatment with Dizocilpine (HY-15084B) or Scopolamine (HY-N0296) reversed amnesia (long-term memory) in Wistar rats[8].
| [IC 50]
5-HT5A Receptor: 8.3 (pKi) | [storage]
Store at +4°C |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|