SB 699551

Selective 5-ht5a antagonist CAS# 864741-95-7

SB 699551

Catalog No. BCC7594----Order now to get a substantial discount!

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Chemical structure

SB 699551

3D structure

Chemical Properties of SB 699551

Cas No. 864741-95-7 SDF Download SDF
PubChem ID 11983346 Appearance Powder
Formula C34H47Cl2N3O M.Wt 584.66
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 25 mM in DMSO and to 10 mM in ethanol
Chemical Name 3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[[4-[4-[(2-phenylethylamino)methyl]phenyl]phenyl]methyl]propanamide;dihydrochloride
SMILES CN(C)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)CNCCC3=CC=CC=C3)C(=O)CCC4CCCC4.Cl.Cl
Standard InChIKey QJMKBIHLMPTYTI-UHFFFAOYSA-N
Standard InChI InChI=1S/C34H45N3O.2ClH/c1-36(2)24-25-37(34(38)21-16-28-10-6-7-11-28)27-31-14-19-33(20-15-31)32-17-12-30(13-18-32)26-35-23-22-29-8-4-3-5-9-29;;/h3-5,8-9,12-15,17-20,28,35H,6-7,10-11,16,21-27H2,1-2H3;2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of SB 699551

DescriptionSelective 5-ht5a receptor antagonist (pKi values are 8.3, < 6.0, < 6.0, < 6.0, < 5.5 and < 5.5 for 5-ht5a, 5-HT1B/D, 5-HT2A, 5-HT2C, 5-HT1A and 5-HT7 receptors respectively).

SB 699551 Dilution Calculator

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SB 699551 Molarity Calculator

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Preparing Stock Solutions of SB 699551

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.7104 mL 8.552 mL 17.104 mL 34.2079 mL 42.7599 mL
5 mM 0.3421 mL 1.7104 mL 3.4208 mL 6.8416 mL 8.552 mL
10 mM 0.171 mL 0.8552 mL 1.7104 mL 3.4208 mL 4.276 mL
50 mM 0.0342 mL 0.171 mL 0.3421 mL 0.6842 mL 0.8552 mL
100 mM 0.0171 mL 0.0855 mL 0.171 mL 0.3421 mL 0.4276 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on SB 699551

SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4 -biphenylyl)methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain.[Pubmed:16846620]

Neuropharmacology. 2006 Sep;51(3):566-77.

This study utilised the selective 5-ht(5A) receptor antagonist, SB-699551-A (3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4 -biphenylyl)methyl]propanamide dihydrochloride), to investigate 5-ht5A receptor function in guinea pig brain. SB-699551-A competitively antagonised 5-HT-stimulated [35S]GTPgammaS binding to membranes from human embryonic kidney (HEK293) cells transiently expressing the guinea pig 5-ht5A receptor (pA2 8.1+/-0.1) and displayed 100-fold selectivity versus the serotonin transporter and those 5-HT receptor subtypes (5-HT(1A/B/D), 5-HT2A/C and 5-HT7) reported to modulate central 5-HT neurotransmission in the guinea pig. In guinea pig dorsal raphe slices, SB-699551-A (1 microM) did not alter neuronal firing per se but attenuated the 5-CT-induced depression in serotonergic neuronal firing in a subpopulation of cells insensitive to the 5-HT1A receptor-selective antagonist WAY-100635 (100 nM). In contrast, SB-699551-A (100 or 300 nM) failed to affect both electrically-evoked 5-HT release and 5-CT-induced inhibition of evoked release measured using fast cyclic voltammetry in vitro. SB-699551-A (0.3, 1 and 3 mg/kg s.c.) did not modulate extracellular levels of 5-HT in the guinea pig frontal cortex in vivo. However, when administered in combination with WAY-100635 (0.3 mg/kg s.c.), SB-699551-A (0.3, 1 or 3 mg/kg s.c.) produced a significant increase in extracellular 5-HT levels. These studies provide evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain.

5-ht5A receptors as a therapeutic target.[Pubmed:16516972]

Pharmacol Ther. 2006 Sep;111(3):707-14.

The 5-ht5A receptor is enigmatic among 5-HT receptors since, although the human receptor was cloned in 1994, until recently, very little has been learnt about the function of the receptor in native tissues. Findings from 5-ht5A receptor mRNA localisation and immunolabelling studies have revealed widespread expression in the CNS, and have provided pointers to the potential functional role(s) of the receptor. The expression of the 5-ht5A receptor in raphe nuclei and in higher brain areas, such as the cerebral cortex and hippocampus, suggests a potential autoreceptor function whilst localisation in the suprachiasmatic nucleus (SCN) suggests a role in circadian rhythm control. Additionally, 5-ht5A receptor knockout mouse phenotyping studies support a role in the control of exploratory behaviour. The lack of understanding of the role of the receptor has been, in part, due to the lack of available selective 5-ht5A receptor ligands. However, a selective 5-ht5A receptor antagonist, 3-cyclopentyl-N-[2-(dimethylamino)ethyl]-N-[(4'-{[(2-phenylethyl)amino]methyl}-4- biphenylyl)methyl]propanamide dihydrochloride (SB-699551-A), has recently been identified which appears to be a useful tool with which to elucidate the physiological function of the receptor. Brain localisation and functional studies to date potentially implicate the receptor in the control of circadian rhythms, mood and cognitive function, whilst gene association studies implicate the receptor in the aetiology of schizophrenia. Although much is still to be learnt about the function of the 5-ht5A receptor, on the basis of these findings, it can be speculated that 5-ht5A receptor-selective ligands might show utility in psychiatric disorders such as schizophrenia and unipolar depression in which cognitive or mood disturbances are a feature.

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