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Chemical Structure| 174635-69-9 Chemical Structure| 174635-69-9

Structure of SB-222200
CAS No.: 174635-69-9

Chemical Structure| 174635-69-9

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SB-222200 is a selective, reversible and competitive antagonist of human NK-3 receptor (Ki=4.4 nM) that effectively crosses the blood-brain barrier.

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Product Details of SB-222200

CAS No. :174635-69-9
Formula : C26H24N2O
M.W : 380.48
SMILES Code : O=C(C1=C(C)C(C2=CC=CC=C2)=NC3=CC=CC=C13)N[C@H](C4=CC=CC=C4)CC
MDL No. :MFCD00944072
InChI Key :MQNYRKWJSMQECI-QFIPXVFZSA-N
Pubchem ID :6604009

Safety of SB-222200

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow-derived macrophages (BMDMs) 10 µM 1 hour SB-222200 inhibits the activation of the NLRP3 inflammasome, reducing IL-1β release. Cell Mol Life Sci. 2023 Jul 27;80(8):230
J774A.1 cells 10 µM 1 hour SB-222200 effectively inhibits the activation of the NLRP3 inflammasome, reducing IL-1β release. Cell Mol Life Sci. 2023 Jul 27;80(8):230
COS-7 cells 0.001–1000 µM 10 minutes To study the antagonistic effect of SB-222200 on tiTac3Ra, results showed that SB-222200 had a strong inhibitory effect on tiTac3Ra with IC50 values of 84.11 μM (tiNKB) and 37.05 μM (tiNKF). Biology (Basel). 2021 Sep 27;10(10):968
Rabbit iris sphincter muscle 0.3-3 µM 120 minutes To evaluate the antagonistic effect of SB-222200 on [MePhe7]-NKB-induced contraction. Results showed that SB-222200 inhibited responses to low concentrations (<1 nM) of [MePhe7]-NKB to a greater extent than responses to higher concentrations (>1 nM) of [MePhe7]-NKB, and made the concentration-effect curves steeper and monophasic. Br J Pharmacol. 1997 Oct;122(3):469-76
Rabbit iris sphincter muscle 30-300 nM 120 minutes To evaluate the antagonistic effect of SB-222200 on senktide-induced contraction. Results showed that SB-222200 antagonized senktide-induced contraction in a surmountable and concentration-dependent manner, with a pA2 value of 7.89. Br J Pharmacol. 1997 Oct;122(3):469-76
Human airway smooth muscle cells (HASM) 100 µM 30 minutes SB-222200, as a selective NK3R antagonist, significantly inhibited senktide-induced inositol phosphate synthesis and intracellular Ca2+ concentration increase. Am J Physiol Lung Cell Mol Physiol. 2008 Mar;294(3):L523-34

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
New Zealand White rabbits Conscious rabbits Intravenous injection 1 and 2 mg/kg Single administration, observed for 30 minutes To evaluate the inhibitory effect of SB-222200 on senktide-induced pupillary constriction. Results showed that SB-222200 significantly inhibited senktide-induced pupillary constriction, with a maximum inhibition of 100%. Br J Pharmacol. 1997 Oct;122(3):469-76
C57BL/6 mice MSU-induced peritonitis Intraperitoneal injection 10, 15, 20 mg/kg Single dose SB-222200 dose-dependently reduced the production of IL-1β and IL-6 in the peritoneal fluid, alleviating MSU-induced peritonitis. Cell Mol Life Sci. 2023 Jul 27;80(8):230
Nile tilapia (Oreochromis niloticus) Adult male tilapia Intraperitoneal injection 100 μg/kg Single injection, observed for 2 hours To study the effect of SB-222200 on LH and FSH release, results showed that SB-222200 significantly reduced LH plasma levels but had no significant effect on FSH levels. Biology (Basel). 2021 Sep 27;10(10):968
CD-1 mice Cocaine-induced hyperactivity model Subcutaneous injection 2.5 or 5 mg/kg Single dose or once daily for 5 days To investigate the effects of SB 222200 on cocaine-induced hyperactivity. Results showed that acute administration of SB 222200 attenuated cocaine-induced stereotypic behavior, while repeated administration enhanced hyperactivity induced by cocaine or a low dose of SKF 82958. Neuropharmacology. 2009 Sep;57(3):295-301
Caenorhabditis elegans Wild-type and mutants Culture medium administration 200 nM Single dose, duration not specified SB222200, a high-affinity human tachykinin receptor antagonist, increased the pharyngeal pumping rate in C. elegans PLoS Biol. 2013 Nov;11(11):e1001712
Female C57Bl6/J mice Ovariectomized (OVX) mice Bilateral intra-MePD administration 4.20 pmol (initial dose) and 8.30 pmol (continuous dose) Initial dose for 5 minutes, continuous dose for 65 minutes To investigate whether SB222200 in the MePD can block the suppressive effect of predator odor (TMT) on LH pulsatility. Results showed that SB222200 completely blocked TMT-induced suppression of LH pulses. J Neuroendocrinol. 2024 May;36(5):e13384
Mice NK1 receptor knockout mice Intravenous injection 5 mg/kg Single dose, experiments conducted 15 minutes after administration To evaluate the effect of SB-222200 on NKB-induced plasma extravasation in the lung, results showed that SB-222200 had no significant effect on NKB-induced plasma extravasation. J Physiol. 2002 Sep 15;543(Pt 3):1007-14
Adult male CD-1 mice Cocaine-induced behavioral sensitization model Subcutaneous injection 5 mg/kg Once daily for 5 days Pretreatment with SB 222200 prevented the development of cocaine-induced behavioral sensitization and blocked the expression of sensitization when administered prior to a cocaine challenge. Additionally, SB 222200 reversed tolerance to increased GSK3 phosphorylation following repeated cocaine administration. J Neurochem. 2010 Nov;115(3):635-42
Spontaneously hypertensive rats (SHR) Spontaneously hypertensive rat model Intracerebroventricular (i.c.v.) or ventral tegmental area (VTA) injection 500 pmol Single injection, effect lasted for 8-10 hours To investigate the antihypertensive effect of SB222200 in spontaneously hypertensive rats and its mechanism. Results showed that SB222200 produced antihypertensive effects via activation of dopamine D2 receptors in the ventral tegmental area. Br J Pharmacol. 2010 Dec;161(8):1868-84
Mice Pregnancy-induced hypertension and proteinuria model Intravenous injection 75 μg/mL Once on gestational day 13 and day 14 SB222200 treatment significantly reduced mean systolic pressure and proteinuria in CRP-infused pregnant mice, improved glomerular and placental damage, and decreased sFlt-1 levels Hypertension. 2015 Feb;65(2):430-9

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.28mL

5.26mL

2.63mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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