Tofenacin hydrochloride

SKU:BHB21903414
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Overview
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Tofenacin hydrochloride (CAS 10488-36-5) is a drug intermediate. Molecular formula C17H22ClNO, molecular weight 291.82 g/mol. Also known as TOF hydrochloride.
CAS Number 10488-36-5
Molecular Weight 291.82 g/mol
Storage See Certificate of Analysis
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Catalog no. Size
HY-W740116-50MG 50 mg
HY-W740116-100MG 100 mg
HY-W740116-250MG 250 mg
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  • Storage: Please store the product under the recommended conditions in the Certificate of Analysis.
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Field Specification
Alternative names TOF hydrochloride
CAS no. 10488-36-5
Applications
  • Functional Assay (In Vitro)
Molecular weight 291.82
Molecular formula C17H22ClNO
SMILES CNCCOC(C1=C(C)C=CC=C1)C2=CC=CC=C2.Cl
Storage Refer to Certificate of Analysis (CoA) for storage conditions
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-W740116
Main SKU BHB21903414
Drug Derivatives & Intermediates

Compound Overview

Tofenacin hydrochloride, also known as TOF hydrochloride, is an orally active, weak anticholinergic compound that can be used to study extrapyramidal symptoms and depressive side effects associated with fluphenazine decanoate use[1][2][3][4]. It has the molecular formula C17H22ClNO and a molecular weight of 291.82 g/mol.

Physical & Chemical Properties

CAS Number 10488-36-5
Molecular Formula C17H22ClNO
Molecular Weight 291.82 g/mol
SMILES CNCCOC(C1=C(C)C=CC=C1)C2=CC=CC=C2.Cl
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping Room temperature in continental US; may vary elsewhere.

Literature Cited

Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.

[1]. Altamura AC, e al. Residual neuroleptic-induced parkinsonian symptoms in schizophrenia. A naturalistic study with orphenadrine. Pharmacopsychiatry. 1989 Nov;22(6):246-9.

[2]. Capstick N, et al. A comparative trial of orphenadrine and tofenacin in the control of depression and extrapyramidal side-effects associated with fluphenazine decanoate therapy. The Journal of international medical research. 1976;4(6):435-40.

[3]. Hespe W, et al. Aspects of the biliary excretion of orphenadrine and its N‑demethylated derivative, tofenacin, in the rat. Eur J Pharmacol. 1970 Dec;13(1):113‑122.

[4]. Mason ST, et al. Chronic and acute administration of typical and atypical antidepressants on activity of brain noradrenaline systems in the rat thiopentone anaesthesia model. Psychopharmacology. 1984;84(3):304-9.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.

In Vivo

In male TNO-Wu rats, Tofenacin (10-25 mg/kg; i.v., i.p.; single dose) hydrochloride (TOF hydrochloride) is excreted extensively in bile; in bile fistula rats, 48.4% of an i.v. 10 mg/kg dose appears in bile over 5 hr, and this excretion depends on rapid biotransformation to conjugated metabolites[3]. In male Sheffield strain rats, Tofenacin (5-25 mg/kg; i.p.; single dose) hydrochloride has no effect on the duration of thiopentone anaesthesia[4]. Likewise, Tofenacin (10-20 mg/kg/day; i.p.; daily; 5-15 days) hydrochloride does not affect the duration of thiopentone anaesthesia in male Sheffield strain rats[4].

Animal ModelTNO-Wu (male, 150-250 g)[3]
Dosage10 mg/kg (labelled, i.v. study); 25 mg/kg (non-radioactive, pretreatment)
Administrationi.v.; single dose; i.p.; single dose, 30 min before labelled dose
ResultExcreted 48.4% of administered radioactivity in bile over 5 hr after i.v. dosing in bile fistula rats. Eliminated 42.2% of administered radioactivity via bile after i.v. dosing in normal rats, exceeding urinary elimination. Reached maximum blood radioactivity concentration immediately, maximum liver radioactivity concentration at 10 min, and maximum bile radioactivity concentration at 15-20 min after i.v. dosing. Exceeded liver radioactivity concentration in bile by 5 min post-dosing, with a maximum bile-to-liver concentration ratio of 7.21 at 20 min. Showed a sharp maximum in biliary excretion of radioactivity in the second 15-min period, followed by prolonged, reduced excretion. Had conjugated metabolites dominate biliary radioactivity even in the first 5 min post-dosing, with free tofenacin accounting for only a small fraction. Decreased biliary excretion of radioactivity in the first hour after administration when pretreated with proadifen. Showed no change in biliary excretion of labelled tofenacin when pretreated with non-radioactive tofenacin.
Animal ModelSheffield strain (male, 250-350 g)[4]
Dosage5 mg/kg; 10 mg/kg; 25 mg/kg
Administrationi.p.; single dose
ResultDid not alter thiopentone anaesthesia duration at any tested dose.
Animal ModelSheffield strain (male, 250-350 g)[4]
Dosage10 mg/kg/day; 20 mg/kg/day
Administrationi.p.; daily; 5 days; 15 days
ResultDid not alter thiopentone anaesthesia duration at any tested dose or administration duration.

Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.

Q.Why is there no price listed?
A.Every size of this product is quoted on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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