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BRL-15572 Dihydrochloride

BRL-15572 Dihydrochloride

ArtNr	S2677-10000
Hersteller	Selleckchem
CAS-Nr.	193611-72-2
Menge	10 g
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 200 mg 5 mg 50 mg 5 g
Kategorie	Metabolism Regulation of Appetite Inhibitors & Compound Libraries Small Molecules
Typ	Inhibitors
Specific against	other
Smiles	C1CN(CCN1CC(C(C2=CC=CC=C2)C3=CC=CC=C3)O)C4=CC(=CC=C4)Cl.Cl.Cl
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	5-HT1D,5-HT Receptor
Similar products	BRL-15572
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	479, 87
Administration	Administered via i.v.
Animal Models	Male Wistar rats with diabetes
Cell lines	CHO cells expressing the h5-HT1B or h5-HT1D receptors
Concentrations	0 uM -10 uM
Dosages	1 mg/kg, 2 mg/kg
Formulation	20% propylene glycol
IC50	7.9 (pKi) [1], 7.9 (pKi) [1], 7.9 (pKi) [1], 7.9 (pKi) [1], 7.9 (pKi) [1], 7.9 (pKi) [1]
In vitro	BRL-15572 displays high affinity and selectivity for h5-HT1D, receptors. BRL-15572 has 60-fold higher affinity for h5-HT1D, than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D, receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP gamma S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities for 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 uM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors. [1] In human atrial appendages, the electrically evoked tritium overflow was inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM, 23 times Ki at h5-HT1D receptors). [2] The inhibitory effect of 5-HT on the K+-evoked overflow of glutamate is antagonized by the h5-HT1D receptor ligand BRL-15572. BRL-15572 (1 uM) is unable to modify the effect of 5-HT at the autoreceptor regulating [3H]5-HT release. [3] The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247. [4]
In vivo	In diabetic pithed rats, administration of the selective 5-HT1D receptor antagonist BRL-15572 (2 mg/kg) does not modify the decreased HR induced by vagal electrical stimulation. The effects of L-694, 247 (50 ug/kg), a selective agonist for non-rodent 5-HT1B and 5-HT1D receptors, on the vagally induced bradycardia are not apparent after pretreatment with BRL-15572. [5]
Incubation Time	30 minutes
Method	[35S]GTPgammaS binding studies. [35S]GTPgammaS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1, 106 cells are preincubated at 30C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl 2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 u M), with or without BRL-15572. The reaction is started by the addition of 10 uL of [35S]GTPgammaS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30C. Non-specific binding is determined by addition of unlabelled GTPgammaS (10 uM), prior to the addition of cells. The reaction is stopped by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Radioactivity is determined by liquid scintillation spectrometry.
Solubility (25C)	DMSO 96 mg/mL, Water <1 mg/mL, Ethanol 40 mg/mL
Information	BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.
Chemical Name	3-(4-(3-chlorophenyl)piperazin-1-yl)-1, 1-diphenylpropan-2-ol dihydrochloride
Features	BRL 15572 is a selective 5-HT1D/1B receptor antagonist.

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