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CAS No. :	1049747-87-6
Formula :	C₂₁H₂₁Cl₃N₄O₂
M.W :	467.78
SMILES Code :	O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3.[H]Cl.[H]Cl
Synonyms :	SB-242084 (hydrochloride); SB 242084 dihydrochloride
MDL No. :	MFCD02684417
InChI Key :	GCMNSEILNIPNSX-UHFFFAOYSA-N
Pubchem ID :	16219981

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

Dorsal raphe serotonin neurons	20 nM	10 minutes	To investigate the role of 5-HT2C receptors in regulating GABA activity during cocaine withdrawal. Bath application of SB 242084 restored cocaine withdrawal-induced heightened GABA activity to baseline levels.	Neuropharmacology. 2015 Jun;93:41-51
CHO-1C19 cells	100 nM	25 minutes	In cells with lower receptor expression levels, SB 242084 had no significant effect on IP accumulation, indicating differential pharmacological properties depending on receptor density.	J Neurosci. 2004 Mar 31;24(13):3235-41
CHO-1C7 cells	100 nM	25 minutes	To evaluate the pharmacological properties of SB 242084 at 5-HT2C receptors, it was found to display weak agonist activity on PLC-dependent responses but full inverse agonist activity on PLA2 and Gαi activation.	J Neurosci. 2004 Mar 31;24(13):3235-41

C57Bl/6J mice	DOI-elicited head-twitch response model	Subcutaneous injection	0.03, 0.3, and 3 mg/kg	Single administration	To evaluate the effect of SB 242084 on DOI-elicited head-twitch response	Neuropharmacology. 2013 Jul;70:112-21
Rats	Spatial reversal learning model	Intracranial infusion	0.1, 0.3, 1.0 μg	Daily, immediately before behavioral testing	To investigate the effects of SB 242084 in OFC, mPFC, and NAc on spatial reversal learning. Results showed that intra-OFC infusions of SB 242084 significantly improved spatial reversal learning by reducing the number of trials to criterion and perseverative errors. No significant effects were observed with intra-mPFC or intra-NAc infusions.	J Neurosci. 2010 Jan 20;30(3):930-8
Rats	Auditory fear conditioning model	Intraperitoneal injection	0.2 mg/kg	Single injection, 60 minutes before testing	To evaluate the blocking effect of SB 242084 on the enhancement of fear expression induced by acute SSRI (citalopram). Results showed that pretreatment with SB 242084 significantly blocked the citalopram-induced enhancement of fear expression.	Biol Psychiatry. 2007 Nov 15;62(10):1111-8
Rats	Fear discrimination model	Intraperitoneal injection	0.25 or 1.0 mg/kg	Once daily for 4 or 5 days	SB 242084 reduced behavioral freezing during conditioning, improved learning and subsequent inhibition of fear by the safety signal. Discrimination was apparent in the first recall test, and discrimination during training was evident after 3 days of conditioning versus 5 days in the vehicle treated controls.	Prog Neuropsychopharmacol Biol Psychiatry. 2016 Feb 4;65:78-84
Swiss-Webster mice	Ketamine-induced hypothermia model	Intraperitoneal injection	0.3 mg/kg	Single administration, temperature recorded for 90 minutes post-administration	To evaluate the effect of SB-242084 on the reversal of ketamine-induced hypothermia by WAY-163909. Results showed that pretreatment with SB-242084 fully reversed the blockade of ketamine-induced hypothermia by WAY-163909.	Eur J Pharmacol. 2019 Jan 5;842:255-261
Zebrafish	Scn1a mutant zebrafish model	Incubation in embryo medium	0.31 μM	22 hours	To explore the anti-epileptic mechanisms of fenfluramine, SB 242084 (5-HT2C receptor antagonist) was able to counteract the FA-induced inhibition of epileptiform activity	Front Pharmacol. 2017 Apr 6;8:191
Mice	Head-twitch response model	Intraperitoneal injection	0.5 mg/kg	Single administration, observed for 20-60 minutes	Tested the effect of SB-242084 on 25CN-NBOH-induced head twitch responses, finding that SB-242084 did not block HTRs induced by 1.5 mg/kg of 25CN-NBOH but increased the number of HTRs at a 3.0 mg/kg dose.	Front Pharmacol. 2018 Feb 6;9:17
Rats	Oxycodone self-administration model	Intraperitoneal injection	0.5 mg/kg	Single administration	SB 242084 blocked the inhibitory effect of lorcaserin on oxycodone intake	ACS Chem Neurosci. 2017 May 17;8(5):1065-1073
Rats	Dopamine agonist-induced oral movements model	Intraperitoneal injection	1 mg/kg	Single administration, observed for 60 minutes	SB 242084 reduced the oral movements induced by quinpirole (0.5 mg/kg)	Int J Mol Sci. 2020 Nov 12;21(22):8509
Rats	Anesthetized rats	Intravenous injection	1 mg/kg	Single dose	To investigate the blocking effect of SB 242084 on WAY 161503-induced inhibition of 5-HT cell firing and confirm its mechanism mediated via 5-HT2C receptors.	Br J Pharmacol. 2006 Dec;149(7):861-9
Rats	EEG-equipped rats	Intraperitoneal injection	1 mg/kg	Single dose	To investigate the effect of SB-242084 on EEG gamma band activity, results showed that acute SB-242084 increased gamma power (30–60 Hz) in light and deep slow-wave sleep, and passive wakefulness.	Front Pharmacol. 2020 Jan 29;10:1636
Male mice	Acute thermal pain models and chemotherapy-evoked neuropathic pain model	Intraperitoneal injection	1 mg/kg	Single administration	To evaluate the effect of SB-242084 on decursinol-induced antinociception, results showed that SB-242084 failed to attenuate decursinol-induced antinociception in the tail-flick assay.	Front Pharmacol. 2022 Sep 29;13:968976
Mice	SERT knockout mice and wild-type littermates	Intraperitoneal injection	1 mg/kg	Single dose	To investigate the role of 5-HT2C receptors in regulating incentive motivation, SB 242084 partially reversed the effects of SERT knockout and citalopram on responding for conditioned reinforcers and unconditioned sensory reinforcers but had no significant effect on responding for saccharin.	Neuropsychopharmacology. 2016 Sep;41(10):2566-76
Rats	Social Affective Preference (SAP) test	Intraperitoneal injection	1 mg/kg	Single dose, 30-40 minutes before testing	Blocking 5-HT2C receptors interfered with the test rats' social preference behaviors toward stressed juvenile and adult conspecifics	Neuropharmacology. 2023 Sep 15;236:109598
Rats	Freely moving rats and anesthetized rats	Intraperitoneal injection	1 mg/kg	Single injection	SB-242084 reversed the inhibitory effect of mCPP on hippocampal theta rhythm	Neuropharmacology. 2011 Sep;61(3):489-94
C57BL/6 mice	Anxiety model produced by cocaine withdrawal	Intraperitoneal injection or intra-DR microinjection	1 mg/kg (i.p.) or 25 nmol (intra-DR)	Administered 24 hours after withdrawal, tested 1 hour later	To evaluate the role of 5-HT2C receptors in regulating anxiety during cocaine withdrawal. Both systemic and intra-DR blockade of 5-HT2C receptors attenuated anxiety-like behavior produced by cocaine withdrawal.	Neuropharmacology. 2015 Jun;93:41-51
Rats	No specific model	Intrastriatal perfusion	1.0 µM	Single administration, lasting 30 minutes	To investigate the effect of SB 242084 on striatal dopamine release, results showed that SB 242084 perfusion increased basal dopamine levels in the striatum.	J Neurochem. 2014 Nov;131(4):432-43
Mice	Morphine-dependent mice model	Intraperitoneal injection	1.0 mg/kg	Single administration	SB 242084 blocked the lorcaserin-mediated suppression of behavioral sensitization and withdrawal symptoms	Neuropharmacology. 2016 Feb;101:246-54
Rats	Methamphetamine self-administration model	Brain slice perfusion	1.0μM	Single administration, lasting at least 5 minutes	To evaluate the blocking effect of SB 242084 on neuronal excitability changes induced by 5-HT2C receptor agonists and inverse agonists. Results showed that SB 242084 blocked the increase in neuronal excitability induced by SB 206553 and Ro 60-0175.	Neuropharmacology. 2015 Feb;89:113-21
Rats	Conscious rats	Bilateral microinjection into the hypothalamic paraventricular nucleus	10 nmol	Single injection, observed for 30 minutes	To investigate the inhibitory effect of SB-242084 on ( /H11002)DOI-induced neuroendocrine responses. Results showed that SB-242084 did not inhibit ( /H11002)DOI-induced increases in oxytocin, prolactin, ACTH, corticosterone, and renin levels.	J Neurosci. 2002 Nov 1;22(21):9635-42
Rats	Anesthetized rats	Intraperitoneal injection	1-10 mg/kg	Single administration	To evaluate the effect of SB 242084 on DA release in the striatum and nucleus accumbens, it was found to dose-dependently increase DA release, though the effect was weaker compared to SB 206553.	J Neurosci. 2004 Mar 31;24(13):3235-41
Rats	MDMA-induced hyperthermia model	Intraperitoneal injection	3 mg/kg	Single dose, 20 minutes before MDMA administration	To investigate the effect of SB 242084 on MDMA-induced hyperthermia. Results showed that SB 242084 did not alter MDMA-induced hyperthermia.	Br J Pharmacol. 2002 Jan;135(1):170-80
Male Wistar rats	Alcohol dependence model	Intraperitoneal injection	3 mg/kg	Once daily for 3 days	Reduced relapse-like drinking behavior but had no effect on circadian phase of alcohol consumption	Neuropsychopharmacology. 2015 Dec;40(13):2897-906
Female Sprague-Dawley rats	Anesthetized rat model	Intravenous injection	30 µg/kg	Single dose	SB 242084 blocked the activation of EUS-EMG signal by Ro 60-0175 but did not block the increase in urethral pressure. Additionally, SB 242084 reversed the inhibitory action of Ro 60-0175 on the micturition reflex.	Br J Pharmacol. 2008 Oct;155(3):343-56

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CAS No.: 1049747-87-6

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CAS No.: 1049747-87-6

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	2.14mL 0.43mL 0.21mL	10.69mL 2.14mL 1.07mL	21.38mL 4.28mL 2.14mL
Dissolving Methods	Animal experiment 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

Precautionary Statements-General
Code	Phrase
P101	If medical advice is needed,have product container or label at hand.
P102	Keep out of reach of children.
P103	Read label before use
Prevention
Code	Phrase
P201	Obtain special instructions before use.
P202	Do not handle until all safety precautions have been read and understood.
P210	Keep away from heat/sparks/open flames/hot surfaces. - No smoking.
P211	Do not spray on an open flame or other ignition source.
P220	Keep/Store away from clothing/combustible materials.
P221	Take any precaution to avoid mixing with combustibles
P222	Do not allow contact with air.
P223	Keep away from any possible contact with water, because of violent reaction and possible flash fire.
P230	Keep wetted
P231	Handle under inert gas.
P232	Protect from moisture.
P233	Keep container tightly closed.
P234	Keep only in original container.
P235	Keep cool
P240	Ground/bond container and receiving equipment.
P241	Use explosion-proof electrical/ventilating/lighting/equipment.
P242	Use only non-sparking tools.
P243	Take precautionary measures against static discharge.
P244	Keep reduction valves free from grease and oil.
P250	Do not subject to grinding/shock/friction.
P251	Pressurized container: Do not pierce or burn, even after use.
P260	Do not breathe dust/fume/gas/mist/vapours/spray.
P261	Avoid breathing dust/fume/gas/mist/vapours/spray.
P262	Do not get in eyes, on skin, or on clothing.
P263	Avoid contact during pregnancy/while nursing.
P264	Wash hands thoroughly after handling.
P265	Wash skin thouroughly after handling.
P270	Do not eat, drink or smoke when using this product.
P271	Use only outdoors or in a well-ventilated area.
P272	Contaminated work clothing should not be allowed out of the workplace.
P273	Avoid release to the environment.
P280	Wear protective gloves/protective clothing/eye protection/face protection.
P281	Use personal protective equipment as required.
P282	Wear cold insulating gloves/face shield/eye protection.
P283	Wear fire/flame resistant/retardant clothing.
P284	Wear respiratory protection.
P285	In case of inadequate ventilation wear respiratory protection.
P231 + P232	Handle under inert gas. Protect from moisture.
P235 + P410	Keep cool. Protect from sunlight.
Response
Code	Phrase
P301	IF SWALLOWED:
P304	IF INHALED:
P305	IF IN EYES:
P306	IF ON CLOTHING:
P307	IF exposed:
P308	IF exposed or concerned:
P309	IF exposed or if you feel unwell:
P310	Immediately call a POISON CENTER or doctor/physician.
P311	Call a POISON CENTER or doctor/physician.
P312	Call a POISON CENTER or doctor/physician if you feel unwell.
P313	Get medical advice/attention.
P314	Get medical advice/attention if you feel unwell.
P315	Get immediate medical advice/attention.
P320
P302 + P352	IF ON SKIN: wash with plenty of soap and water.
P321
P322
P330	Rinse mouth.
P331	Do NOT induce vomiting.
P332	IF SKIN irritation occurs:
P333	If skin irritation or rash occurs:
P334	Immerse in cool water/wrap n wet bandages.
P335	Brush off loose particles from skin.
P336	Thaw frosted parts with lukewarm water. Do not rub affected area.
P337	If eye irritation persists:
P338	Remove contact lenses, if present and easy to do. Continue rinsing.
P340	Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P341	If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P342	If experiencing respiratory symptoms:
P350	Gently wash with plenty of soap and water.
P351	Rinse cautiously with water for several minutes.
P352	Wash with plenty of soap and water.
P353	Rinse skin with water/shower.
P360	Rinse immediately contaminated clothing and skin with plenty of water before removing clothes.
P361	Remove/Take off immediately all contaminated clothing.
P362	Take off contaminated clothing and wash before reuse.
P363	Wash contaminated clothing before reuse.
P370	In case of fire:
P371	In case of major fire and large quantities:
P372	Explosion risk in case of fire.
P373	DO NOT fight fire when fire reaches explosives.
P374	Fight fire with normal precautions from a reasonable distance.
P376	Stop leak if safe to do so. Oxidising gases (section 2.4) 1
P377	Leaking gas fire: Do not extinguish, unless leak can be stopped safely.
P378
P380	Evacuate area.
P381	Eliminate all ignition sources if safe to do so.
P390	Absorb spillage to prevent material damage.
P391	Collect spillage. Hazardous to the aquatic environment
P301 + P310	IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P301 + P312	IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P301 + P330 + P331	IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P302 + P334	IF ON SKIN: Immerse in cool water/wrap in wet bandages.
P302 + P350	IF ON SKIN: Gently wash with plenty of soap and water.
P303 + P361 + P353	IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P304 + P312	IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell.
P304 + P340	IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P304 + P341	IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338	IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P306 + P360	IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes.
P307 + P311	IF exposed: call a POISON CENTER or doctor/physician.
P308 + P313	IF exposed or concerned: Get medical advice/attention.
P309 + P311	IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.
P332 + P313	IF SKIN irritation occurs: Get medical advice/attention.
P333 + P313	IF SKIN irritation or rash occurs: Get medical advice/attention.
P335 + P334	Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages.
P337 + P313	IF eye irritation persists: Get medical advice/attention.
P342 + P311	IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.
P370 + P376	In case of fire: Stop leak if safe to Do so.
P370 + P378	In case of fire:
P370 + P380	In case of fire: Evacuate area.
P370 + P380 + P375	In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion.
P371 + P380 + P375	In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion.
Storage
Code	Phrase
P401
P402	Store in a dry place.
P403	Store in a well-ventilated place.
P404	Store in a closed container.
P405	Store locked up.
P406	Store in corrosive resistant/ container with a resistant inner liner.
P407	Maintain air gap between stacks/pallets.
P410	Protect from sunlight.
P411
P412	Do not expose to temperatures exceeding 50 oC/ 122 oF.
P413
P420	Store away from other materials.
P422
P402 + P404	Store in a dry place. Store in a closed container.
P403 + P233	Store in a well-ventilated place. Keep container tightly closed.
P403 + P235	Store in a well-ventilated place. Keep cool.
P410 + P403	Protect from sunlight. Store in a well-ventilated place.
P410 + P412	Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF.
P411 + P235	Keep cool.
Disposal
Code	Phrase
P501	Dispose of contents/container to ...
P502	Refer to manufacturer/supplier for information on recovery/recycling

Physical hazards
Code	Phrase
H200	Unstable explosive
H201	Explosive; mass explosion hazard
H202	Explosive; severe projection hazard
H203	Explosive; fire, blast or projection hazard
H204	Fire or projection hazard
H205	May mass explode in fire
H220	Extremely flammable gas
H221	Flammable gas
H222	Extremely flammable aerosol
H223	Flammable aerosol
H224	Extremely flammable liquid and vapour
H225	Highly flammable liquid and vapour
H226	Flammable liquid and vapour
H227	Combustible liquid
H228	Flammable solid
H229	Pressurized container: may burst if heated
H230	May react explosively even in the absence of air
H231	May react explosively even in the absence of air at elevated pressure and/or temperature
H240	Heating may cause an explosion
H241	Heating may cause a fire or explosion
H242	Heating may cause a fire
H250	Catches fire spontaneously if exposed to air
H251	Self-heating; may catch fire
H252	Self-heating in large quantities; may catch fire
H260	In contact with water releases flammable gases which may ignite spontaneously
H261	In contact with water releases flammable gas
H270	May cause or intensify fire; oxidizer
H271	May cause fire or explosion; strong oxidizer
H272	May intensify fire; oxidizer
H280	Contains gas under pressure; may explode if heated
H281	Contains refrigerated gas; may cause cryogenic burns or injury
H290	May be corrosive to metals
Health hazards
Code	Phrase
H300	Fatal if swallowed
H301	Toxic if swallowed
H302	Harmful if swallowed
H303	May be harmful if swallowed