1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. SB-616234-A

SB-616234-A 

Cat. No.: HY-19477 Purity: 98.14%
Handling Instructions

SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

For research use only. We do not sell to patients.

SB-616234-A Chemical Structure

SB-616234-A Chemical Structure

CAS No. : 908601-49-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 821 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5850 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.

IC50 & Target

5-HT1B Receptor

 

In Vitro

SB-616234-A possesses high affinity for human 5-HT1B receptors stably expressed in Chinese hamster ovary (CHO) cells (pKi 8.3 ± 0.2), and is over 100-fold selective for a range of molecular targets except h5-HT1D receptors (pKi 6.6 ± 0.1). Similarly, affinity (pKi) for rat and guinea pig striatal 5-HT1B receptors is 9.2 ± 0.1. In [35S]-GTPγS binding studies in the human recombinant cell line, SB-616234-A acts as a high affinity antagonist with a pA2 value of 8.6 ± 0.2 whilst providing no evidence of agonist activity in this system. In [35S]-GTPγS binding studies in rat striatal membranes, SB-616234-A acts as a high affinity antagonist with an apparent pKB of 8.4 ± 0.5, again whilst providing no evidence of agonist activity in this system. SB-616234-A (1 μM) potentiates electrically stimulated [3H]-5-HT release from guinea pig and rat cortical slices (S2/S1 ratios of 1.8 and 1.6, respectively)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SB-616234-A reverses the 5-HT1/7 receptor agonist, SKF-99101H-induced hypothermia in guinea pigs in a dose related manner with an ED50 of 2.4 mg/kg p.o. SB-616234-A produces dose-related anxiolytic effects in both rat and guinea pig maternal separation-induced vocalisation models with an ED50 of 1.0 and 3.3 mg/kg i.p., respectively[1]. SB-616234-A (0.3-30 mg/kg p.o.) causes a dose-dependent inhibition of ex vivo [3H]-GR125743 binding to rat striatal 5-HT1B receptors with an ED50 of 2.83 ± 0.39 mg/kg p.o[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

574.11

Formula

C₃₂H₃₆ClN₅O₃

CAS No.

908601-49-0

SMILES

O=C(N1CCC2=C1C=C(N3C[[email protected]@H](C)N[[email protected]@H](C)C3)C(OC)=C2)C4=CC=C(C5=CC=C(C6=NOC(C)=N6)C=C5C)C=C4.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 10 mg/mL (17.42 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7418 mL 8.7091 mL 17.4183 mL
5 mM 0.3484 mL 1.7418 mL 3.4837 mL
10 mM 0.1742 mL 0.8709 mL 1.7418 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Seven days post surgery animals are placed in microdialysis cages for overnight habituation prior to microdialysis experimentation. The following morning microdialysis probes (2 mm cuprophane membrane) are implanted, via the guide cannulae, into the frontal cortex and/or dentate gyrus. Probes are perfused with artificial cerebrospinal fluid (aCSF) containing NaCl 145 mM, KCl 2.7 mM, MgCl2 1.0 mM, CaCl2 1.2 mM, Na2HPO4 2.0 mM (pH 7.4) at a flow rate of 1 μL/min. A 30 min sampling regime is used throughout the microdialysis procedure. Following a 2 h equilibration period, 3 microdialysis samples are collected to establish basal extracellular levels of 5-HT. Guinea pigs are then dosed with vehicle (1% methyl cellulose, 1 mg/kg p.o.), paroxetine (3 mg/kg p.o.) or SB-616234-A (3, 10 or 30 mg/kg p.o.). Microdialysis samples are collected for a further 5 h following drug administration. 5-HT content of microdialysate samples is measured using high performance liquid chromatography (HPLC) with electrochemical detection (ECD). At the end of the experiment probes are removed and animals return to their home cage. Animals are re-used in a randomised cross-over design with 7 days between uses and a maximum of 4 uses per subject.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

SB-616234-A5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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SB-616234-A
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