Granisetron hydrochloride

Modify Date: 2024-01-02 19:26:11

Granisetron hydrochloride structure	Common Name	Granisetron hydrochloride
	CAS Number	107007-99-8	Molecular Weight	348.870
	Density	1.33g/cm3	Boiling Point	532ºC at 760mmHg
	Molecular Formula	C₁₈H₂₅ClN₄O	Melting Point	290-292°C
	MSDS	Chinese USA	Flash Point	275.6ºC
	Symbol	GHS07	Signal Word	Warning

Use of Granisetron hydrochloride

Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.IC50 Value: 17uM (GR reduced 5-HT-evoked contractions) [1]Target: 5-HT3 receptorin vitro: In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT [1].in vivo: Leukocyte accumulation was dose-dependently inhibited by granisetron both at 6 and 72 h after induction of inflammation. Granisetron increased PGE(2) level at a lower dose (50 microg/pouch) but higher doses (100 and 200 microg/pouch) inhibited the release. At the same time, TNFalpha production was decreased by the lower dose and increased by higher doses of granisetron in a reciprocal fashion [2]. The GTDS displayed non-inferiority to oral granisetron: complete control was achieved by 60% of patients in the GTDS group, and 65% in the oral granisetron group (treatment difference, -5%; 95% confidence interval, -13-3). Both treatments were well tolerated, the most common adverse event being constipation [3].Clinical trial: Effect of External Heat on a Transdermal Granisetron Patch in Pharmacokinetics (PK) of Healthy Subjects. Phase 1

Name	Granisetron hydrochloride
Synonym	More Synonyms

Description	Granisetron Hcl(BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.IC50 Value: 17uM (GR reduced 5-HT-evoked contractions) [1]Target: 5-HT3 receptorin vitro: In rat forestomach GR reduced 5-HT-evoked contractions at IC50 17 /- 6 uM. In isolated rabbit heart, GR 0.003-0.03 nM dose-dependently reduced s-HT tachycardia; at high levels GR reduced submaximal and maximal responses to 5-HT [1].in vivo: Leukocyte accumulation was dose-dependently inhibited by granisetron both at 6 and 72 h after induction of inflammation. Granisetron increased PGE(2) level at a lower dose (50 microg/pouch) but higher doses (100 and 200 microg/pouch) inhibited the release. At the same time, TNFalpha production was decreased by the lower dose and increased by higher doses of granisetron in a reciprocal fashion [2]. The GTDS displayed non-inferiority to oral granisetron: complete control was achieved by 60% of patients in the GTDS group, and 65% in the oral granisetron group (treatment difference, -5%; 95% confidence interval, -13-3). Both treatments were well tolerated, the most common adverse event being constipation [3].Clinical trial: Effect of External Heat on a Transdermal Granisetron Patch in Pharmacokinetics (PK) of Healthy Subjects. Phase 1
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease
References	[1]. Sanger GJ, Nelson DR. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur J Pharmacol. 1989 Jan 10;159(2):113-24. [2]. Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou A, The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation. Int Immunopharmacol. 2010 Sep;10(9):1010-6. [3]. Boccia RV, Gordan LN, Clark G, Efficacy and tolerability of transdermal granisetron for the control of chemotherapy-induced nausea and vomiting associated with moderately and highly emetogenic multi-day chemotherapy: a randomized, double-blind, phase III

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Research Areas >> Neurological Disease

References

[1]. Sanger GJ, Nelson DR. Selective and functional 5-hydroxytryptamine3 receptor antagonism by BRL 43694 (granisetron). Eur J Pharmacol. 1989 Jan 10;159(2):113-24.

[2]. Maleki-Dizaji N, Eteraf-Oskouei T, Fakhrjou A, The effects of 5HT3 receptor antagonist granisetron on inflammatory parameters and angiogenesis in the air-pouch model of inflammation. Int Immunopharmacol. 2010 Sep;10(9):1010-6.

[3]. Boccia RV, Gordan LN, Clark G, Efficacy and tolerability of transdermal granisetron for the control of chemotherapy-induced nausea and vomiting associated with moderately and highly emetogenic multi-day chemotherapy: a randomized, double-blind, phase III

Density	1.33g/cm3
Boiling Point	532ºC at 760mmHg
Melting Point	290-292°C
Molecular Formula	C₁₈H₂₅ClN₄O
Molecular Weight	348.870
Flash Point	275.6ºC
Exact Mass	348.171692
PSA	50.16000
LogP	3.44920
Vapour Pressure	0mmHg at 25°C
Index of Refraction	1.69
Storage condition	Room temp

Granisetron Hydrochloride Revision number: 5
SAFETY DATA SHEET

Section1. IDENTIFICATION
Product name:Granisetron Hydrochloride

Revision number:5

Section2. HAZARDS IDENTIFICATION
GHS classification
PHYSICAL HAZARDSNot classified
HEALTH HAZARDS
Acute toxicity (Oral)Category 4
Not classified
ENVIRONMENTAL HAZARDS
GHS label elements, including precautionary statements
Pictograms or hazard symbols
Signal wordWarning
Hazard statementsHarmful if swallowed
Precautionary statements:
[Prevention]Do not eat, drink or smoke when using this product.
Wash hands thoroughly after handling.
IF SWALLOWED: Call a POISON CENTER or doctor/physician if you feel unwell.
[Response]
Rinse mouth.
Dispose of contents/container through a waste management company authorized by
[Disposal]
the local government.

Section3. COMPOSITION/INFORMATION ON INGREDIENTS
Substance/mixture:Substance
Components:Granisetron Hydrochloride
Percent:>98.0%(LC)(T)
CAS Number:107007-99-8
Synonyms:1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-
carboxamide Hydrochloride
Chemical Formula:C18H24N4O·HCl

Section4. FIRST AID MEASURES
Inhalation:Remove victim to fresh air and keep at rest in a position comfortable for breathing.
Get medical advice/attention if you feel unwell.
Skin contact:Remove/Take off immediately all contaminated clothing. Rinse skin with
water/shower. If skin irritation or rash occurs: Get medical advice/attention.
Granisetron Hydrochloride

Section4. FIRST AID MEASURES
Eye contact:Rinse cautiously with water for several minutes. Remove contact lenses, if present
and easy to do. Continue rinsing. If eye irritation persists: Get medical
advice/attention.
Ingestion:Call a POISON CENTER or doctor/physician if you feel unwell. Rinse mouth.
Protection of first-aiders:A rescuer should wear personal protective equipment, such as rubber gloves and air-
tight goggles.

Section5. FIRE-FIGHTING MEASURES
Dry chemical, foam, water spray, carbon dioxide.
Suitable extinguishing
media:
Precautions for firefighters: Fire-extinguishing work is done from the windward and the suitable fire-extinguishing
method according to the surrounding situation is used. Uninvolved persons should
evacuate to a safe place. In case of fire in the surroundings: Remove movable
containers if safe to do so.
Special protectiveWhen extinguishing fire, be sure to wear personal protective equipment.
equipment for firefighters:

Section6. ACCIDENTAL RELEASE MEASURES
Personal precautions,Use personal protective equipment. Keep people away from and upwind of spill/leak.
protective equipment and Entry to non-involved personnel should be controlled around the leakage area by
emergency procedures: roping off, etc.
Environmental precautions: Prevent product from entering drains.
Methods and materials for Sweep dust to collect it into an airtight container, taking care not to disperse it.
containment and cleaning Adhered or collected material should be promptly disposed of, in accordance with
up: appropriate laws and regulations.

Section7. HANDLING AND STORAGE
Precautions for safe handling
Technical measures:Handling is performed in a well ventilated place. Wear suitable protective equipment.
Prevent dispersion of dust. Wash hands and face thoroughly after handling.
Use a local exhaust if dust or aerosol will be generated.
Advice on safe handling: Avoid contact with skin, eyes and clothing.
Conditions for safe storage, including any
incompatibilities
Storage conditions:Keep container tightly closed. Store in a cool and dark place.
Store away from incompatible materials such as oxidizing agents.
Packaging material:Comply with laws.

Section8. EXPOSURE CONTROLS / PERSONAL PROTECTION
Engineering controls:Install a closed system or local exhaust as possible so that workers should not be
exposed directly. Also install safety shower and eye bath.
Personal protective equipment
Respiratory protection: Dust respirator. Follow local and national regulations.
Hand protection:Protective gloves.
Eye protection:Safety glasses. A face-shield, if the situation requires.
Skin and body protection: Protective clothing. Protective boots, if the situation requires.

Section9. PHYSICAL AND CHEMICAL PROPERTIES
Solid
Physical state (20°C):
Form:Crystal- Powder
Colour:White - Almost white
No data available
Odour:
pH: No data available
Melting point/freezing point:292°C (dec.)
Boiling point/range:No data available
No data available
Flash point:
Granisetron Hydrochloride

Section9. PHYSICAL AND CHEMICAL PROPERTIES
Flammability or explosive
limits:
Lower:No data available
Upper:No data available
Relative density:No data available
Solubility(ies):
[Water]No data available
No data available
[Other solvents]

Section10. STABILITY AND REACTIVITY
Chemical stability:Stable under proper conditions.
Possibility of hazardous No special reactivity has been reported.
reactions:
Incompatible materials: Oxidizing agents
Hazardous decomposition Carbon monoxide, Carbon dioxide, Nitrogen oxides (NOx), Hydrogen chloride
products:

Section11. TOXICOLOGICAL INFORMATION
orl-rat LD50:350 mg/kg
Acute Toxicity:
ivn-rat LD50:14 mg/kg
Skin corrosion/irritation: No data available
Serious eyeNo data available
damage/irritation:
Germ cell mutagenicity: mmo-sat 5 gm/L (+S9)
cyt-hmn-lym 1500 mg/L
Carcinogenicity:
No data available
IARC =
NTP =No data available
No data available
Reproductive toxicity:
RTECS Number:NK7882200

Section12. ECOLOGICAL INFORMATION
Ecotoxicity:
Fish:No data available
Crustacea:No data available
Algae:No data available
Persistence / degradability: No data available
No data available
Bioaccumulative
potential(BCF):
Mobility in soil
Log Pow:No data available
Soil adsorption (Koc):No data available
Henry's LawNo data available
constant(PaM3/mol):

Section13. DISPOSAL CONSIDERATIONS
Recycle to process, if possible. Consult your local regional authorities. You may be able to dissolve or mix material
with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber system.
Observe all federal, state and local regulations when disposing of the substance.

Section14. TRANSPORT INFORMATION
Hazards Class:Does not correspond to the classification standard of the United Nations
UN-No:Not listed
Granisetron Hydrochloride

Section15. REGULATORY INFORMATION
Safe management ordinance of dangerous chemical product (State Council announces on January 26, 2002
and revised on February 16,2011): Safe use and production, the storage of a dangerous chemical, transport,
loading and unloading were prescribed.

SECTION 16 - ADDITIONAL INFORMATION
N/A

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NK7882200

CHEMICAL NAME :: 1H-Indazole-3-carboxamide, 1-methyl-N-(9-methyl-9-azabicyclo(3.3.1)non-3-yl)-, monohydrochloride, endo-

CAS REGISTRY NUMBER :: 107007-99-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C18-H24-N4-O.Cl-H

MOLECULAR WEIGHT :: 348.92

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 350 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Behavioral - muscle contraction or spasticity

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 350 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 17 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 3 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - tremor Gastrointestinal - nausea or vomiting

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4500 mg/kg/30D-I

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in leukocyte (WBC) count Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18200 mg/kg/26W-I

TOXIC EFFECTS :: Liver - changes in liver weight Blood - changes in platelet count Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 325 mg/kg/30D-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - ptosis Behavioral - tremor

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 52 mg/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating - 19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 1500 mg/L

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 24,6795,1990

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Precautionary Statements	P301 + P312 + P330
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes	Xn: Harmful;Xi: Irritant;
Risk Phrases	R22
Safety Phrases	26-36-37
RIDADR	NONH for all modes of transport
RTECS	NK7882200
HS Code	2933990090

exo-3-Amino-9-m...

CAS#:76272-41-8

1-METHYL-1H-IND...

CAS#:106649-02-9

Granisetron hyd...

CAS#:107007-99-8

Literature: US4886808 A1, ;

Granisetron

CAS#:109889-09-0

~74%

Granisetron hyd...

CAS#:107007-99-8

Literature: INKE, S.A. Patent: WO2008/151677 A1, 2008 ; Location in patent: Page/Page column 13 ;

Precursor 3
CAS#:109889-09-0 Granisetron CAS#:76272-41-8 exo-3-Amino-9-m... CAS#:106649-02-9 1-METHYL-1H-IND...
DownStream 1
CAS#:109889-09-0 Granisetron

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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Due to its distinct pharmacological profile and lower incidence of adverse events compared with other opioids, buprenorphine is considered a safe option for pain and substitution therapy. However, des...

In vitro percutaneous absorption enhancement of granisetron by chemical penetration enhancers.

Drug Dev. Ind. Pharm. 39(4) , 561-8, (2013)

Granisetron (GRN), a potent antiemetic agent, is frequently used to prevent nausea and vomiting induced by cancer cytotoxic chemotherapy and radiation therapy.As part of our efforts to further modify ...

Comparison of the efficacy of ondansetron and granisetron to prevent postoperative nausea and vomiting after laparoscopic cholecystectomy: a systematic review and meta-analysis.

Surg. Laparosc. Endosc. Percutan. Tech. 23(1) , 79-87, (2013)

Our purpose was to assess the prophylactic antiemetic effects of ondansetron versus granisetron for laparoscopic cholecystectomy.We searched Medline, Cochrane Central Register of Controlled Trials, Pu...

Granisetron hydrochloride

1-méthyl-N-[(3-endo)-9-méthyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide chlorhydrate

1H-Indazole-3-carboxamide, 1-methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-, hydrochloride (1:1)

1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide hydrochloride (1:1)

1H-indazole-3-carboxamide, 1-methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-, monohydrochloride

MFCD01747034

Granisetron HCl

1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide hydrochloride

1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide

1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide,hydrochloride

1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazol-3-carboxamidhydrochlorid

Granisetron (Hydrochloride)

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