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Granisetron

Catalog No.
A3443
Serotonin 5-HT3 receptor antagonist
Grouped product items
SizePriceStock Qty
50mg
$90.00
In stock
100mg
$151.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Description: IC50 Value: 17uM (GR reduced 5-HT-evoked contractions) [1] Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. in 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

Chemical Properties

StorageStore at -20°C
M.Wt312.41
Cas No.109889-09-0
FormulaC18H24N4O
Solubility≥25.1 mg/mL in DMSO; ≥12.58 mg/mL in EtOH with ultrasonic; insoluble in H2O
Chemical Name1-methyl-N-[(1S,5R)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide
Canonical SMILESC(N[C@H]1C[C@@]2(N(C)[C@](C1)(CCC2)[H])[H])(=O)C=3C=4C(N(C)N3)=CC=CC4
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

User Guide

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