Structure of SB-222200
CAS No.: 174635-69-9
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
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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Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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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 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
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 |
Tags: SB-222200 | SB222200 | SB 222200 | Neurokinin Receptor | NK receptor | Tachykinin receptor | NK-3R | neurokinin-B | NKB | central | nervous | CNS | penetrant | disorders | inhibitor | 174635-69-9 |
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H201 | Explosive; mass explosion hazard |
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H311 | Toxic in contact with skin |
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H313 | May be harmful in contact with skin |
H314 | Causes severe skin burns and eye damage |
H315 | Causes skin irritation |
H316 | Causes mild skin irritation |
H317 | May cause an allergic skin reaction |
H318 | Causes serious eye damage |
H319 | Causes serious eye irritation |
H320 | Causes eye irritation |
H330 | Fatal if inhaled |
H331 | Toxic if inhaled |
H332 | Harmful if inhaled |
H333 | May be harmful if inhaled |
H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
H335 | May cause respiratory irritation |
H336 | May cause drowsiness or dizziness |
H340 | May cause genetic defects |
H341 | Suspected of causing genetic defects |
H350 | May cause cancer |
H351 | Suspected of causing cancer |
H360 | May damage fertility or the unborn child |
H361 | Suspected of damaging fertility or the unborn child |
H361d | Suspected of damaging the unborn child |
H362 | May cause harm to breast-fed children |
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H371 | May cause damage to organs |
H372 | Causes damage to organs through prolonged or repeated exposure |
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H400 | Very toxic to aquatic life |
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H411 | Toxic to aquatic life with long-lasting effects |
H412 | Harmful to aquatic life with long-lasting effects |
H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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