Nicotredole

Nicotredole (Tryptamide) is an orally active anti-inflammatory and analgesic agent. Nicotredole exhibits evident antiinflammatory effects of potency comparable with Phenylbutazone. Nicotredole has only weak ulcerogenic activity[1][2][3].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

Nicotredole inhibits prostaglandin synthetase activity in vitro[1].

Nicotredole produces antiinflammatory effects in carrageenin-induced rat paw oedema[1]. Nicotredole reverses pyrogen-induced hyperthermia in rats, elicits analgesic effects in rats, prolongs the time of hexobarbital sleep in rats and inhibits locomotor activity in rats and mice[1]. Nicotredole (i.p.) has LD50s of 1260 mg/kg and 1980 mg/kg for male rats and male mice, respectively[1]. Nicotredole (p.o.) has LD50s of 8.5 g/kg and 9.3 g/kg for male rats and male mice, respectively[1]. Nicotredole (25 mg/kg; p.o. or i.p.) undergoes fast absorption (t1/2=4.92-17.5 min) and elimination (t1/2=55.72-74.52 min), can reach Cmax (11-13 μg/cm3) after 30 min, and gives AUC values in the range of 21.40-27.30 (μg•h/cm3)[2].

[1]. Herman ZS, et, al. Basic pharmacological properties of a novel antiinflammatory drug tryptamide. Pol J Pharmacol Pharm. Nov-Dec 1987;39(6):729-36.

[2]. Szumiło H. Pharmacokinetics of tryptamide following oral and intraperitoneal administration in rats. Acta Pol Pharm. 1990;47(1-2):19-22.

[3]. Kulig D, et, al. A comparison of anti-inflammatory, analgesic and ulcerogenic action of tryptamide, ibuprofen and piroxicam. Pol J Pharmacol Pharm. Nov-Dec 1987;39(6):769-72.

DATA ITEMS CITED :

3

MOLECULAR FORMULA :

C16-H15-N3-O

MOLECULAR WEIGHT :

265.34

WISWESSER LINE NOTATION :

T56 BMJ D2MV- CT6NJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1250 mg/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity)

REFERENCE :

DPHFAK Dissertationes Pharmaceuticae et Pharmacologicae. (Warsaw, Poland) V.18-24, 1966-72. For publisher information, see PJPPAA. Volume(issue)/page/year: 22,313,1970 ** REPRODUCTIVE DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

90 mg/kg

SEX/DURATION :

female 6-14 day(s) after conception

TOXIC EFFECTS :

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

REFERENCE :

PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,779,1987

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

DOSE :

4500 mg/kg

SEX/DURATION :

female 6-14 day(s) after conception

TOXIC EFFECTS :

Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :

PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,779,1987