Inhibitors, Agonists, Screening Libraries
www.MedChemExpress.com
Data Sheet
Product Name:Cat. No.:CAS No.:
Molecular Formula:Molecular Weight:Target:Pathway:Solubility:
SB–2242 hydrochlorideHY-101105A180084-26-8C32H33ClN4O3557.085–HT Receptor
GPCR/G Protein; Neuronal SignalingDMSO
BIOLOGICAL ACTIVITY:
SB–2242 hydrochloride is a selective 5–HT1B receptor antagonist, with anxiolytic effect.IC50 & Target: 5–HT1B receptor[2]
In Vitro: SB–2242 has specific toxin–blocking ability and does not inhibit Cho1p. SB–2242 (100 μM–25 μM) shows consistent
efficacy at producing Pap–A resistance. SB–2242 does not directly inhibit the PS synthase enzyme in this in vitro assay. Moreover,SB–2242 specifically blocks the activity of papuamides and not other membrane disruptors. SB–2242 is unable to protectreceptors and displays more than 80 fold selectivity over the closely related 5–HT1D receptor and a range of other receptors.SB–2242 is a potent antagonist with pEC50 of 7.9±0.1. SB–2242 evokes a parallel rightward shift in the 5–HT concentrationresponse curve with pA2 of 8.4±0.2. SB–2242 (100 nM and 1 μM) also significantly increases [3H]–5HT release in electricallystimulated guinea–pig brain cortex slices[3].
wild–type cells against KF, but it is able to provide protection against TPap–A[1]. SB–2242 has a pKi of 8 at human cloned 5–HT1B
In Vivo: SB–2242 (SB 2242) alone or in combination with cocaine, increases anxiety–like behavior. SB 2242 significantly reduces
the amount of locomotor activity in the cocaine–treated rats. SB 2242–treated animals spend a significantly longer time in thecorners than those treated with vehicle[2]. SB 2242 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F–99101–inducedhypothermia in the guinea–pig. SB 2242 (4 mg/kg, p.o) reverses sumatriptan–induced inhibition of 5–HT release showing that it isalso a potent terminal 5–HT autoreceptor antagonist in vivo. SB 2242 (2–16 mg/kg, p.o) does not increase 5–HT levels in thefuinea–pig frontal cortex. However, SB 2242 (4 mg/kg, p.o) causes a significantly increase in levels of 5–HT in the fuinea–pig dentategyrus[3].
PROTOCOL (Extracted from published papers and Only for reference)
Animal Administration: SB–2242 is formulated in a vehicle of 10% Trappsol in sterile water.[2]Ninety minutes before each animal istested, it receives an ip injection of either 5 mg/kg SB 2242 in a vehicle of 10% Trappsol in sterile water or vehicle alone (totalvolume 1 mL/kg). This dosage of this drug is effective as a pharmacological agent. The rat is put back in its home cage until justbefore it is to be tested.
References:
[1]. Cassilly CD, et al. SB–2242 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A. PLoS One. 2016 May 16;11(5):e0154932.[2]. Hoplight BJ, et al. The effects of SB 2242 on anxiety and cocaine–related behaviors in a novel object task. Physiol Behav. 2005 Apr 13;84(5):707–14.Epub 2005 Apr 13.
[3]. Gaster LM, et al. The selective 5–HT1B receptor inverse agonist SB–2242, potently blocks terminal 5–HT autoreceptor function both in vitro and in vivo.
www.MedChemExpress.com
Ann N Y Acad Sci. 1998 Dec 15;861:270–1.
Caution: Product has not been fully validated for medical applications. For research use only.
Tel: 609-228-68 Fax: 609-228-5909 E-mail: tech@MedChemExpress.com
Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
www.MedChemExpress.com
