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1-MICA 50890-83-0

IUPAC Name: 1-methylindazole-3-carboxylic acid
Molecular Weight: 176.17
Molecular Formula: C9H8N2O2
Quality Standard:

    Product Specification

    Description:

    White or pale yellow powder

    Identification:

    By HPLC: The retention time of major peak should match with standard

    Melting range:

    Between 213 ~ 218℃

    Loss on drying:

    NMT 0.5%

    Impurities (HPLC):

    ICA NMT 0.3%、2-MICA NMT 1.5%、Any other NMT 0.5%、Total impurities NMT 2.0%

    Assay by titration( as is):

    Between 97.0 ~ 101.0%

    description1

    PRODUCT DESCRIPTION

    The goal of antiemetic therapy is to prevent or reduce the frequency and intensity of nausea and vomiting associated with chemotherapy. Early antiemetic drugs used in clinical practice had severe nerve center inhibition or extrapyramidal adverse reactions. Therefore, a variety of highly selective 5-ht3 receptor blockers have been developed since the 1980s and gradually develop into the mainstream drugs for the treatment of nausea and vomiting caused by chemotherapy. Based on the mechanism, antiemetic drugs can be divided into dopamine blockers, vomiting central in the and nk-1 receptor blockers.

    Following the introduction of the first generation of highly selective 5-HT3 receptor blockers, such as Ondansetron, a number of derivatives of these drugs have been utilized clinically, including Granisetron, Navoban, and Azasetron, with proven curative effects and fewer side effects.

    Mechanisms: The mechanisms underlying nausea and vomiting brought on by chemotherapy are quite intricate and mostly consist of the following elements: Chemotherapeutic drugs and their metabolites stimulate and activate the vomiting center, causing vomiting; various toxic substances in blood can act on the vomiting center, unprotected by the blood-brain barrier, and the signal can be passed to the vomiting center, causing vomiting; the majority of cytotoxic drugs can stimulate the gastrointestinal mucosa, causing mucosa damage and leading the chromaffin cells on mucous membrane, especially from the stomach to the ileal mucosa, to release 5-HT, which combines the 5-HT3 receptor to generate nerve impulses spreading to the vomiting center, forming vomit The dopaminergic, histaminergic, muscarinergic, and 5-HT3 receptors). 

    The majority of antiemetic medications also function by binding to one or more receptors. An essential central transmitter in the human body is 5-HT. There are four different forms of its receptor: 5-HT1, 5-HT2, 5-HT3, 5-HT4, and a few subtypes. 5 - HT3 receptor blockers can be given to the vagus nerve's 5-HT3 receptors to prevent vomiting by acting on the receptors, which blocks the afferent impulse that would otherwise cause vomiting and inhibits the excitement of vagal fibers and the activation of AP and NTS 5-HT3.