Detail of "59729-33-8"

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CAS Number:
59729-33-8
Name:
5-Isobenzofurancarbonitrile,1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-
Superlist Name:
Citalopram
Molecular Structure:
Formula:
C₂₀H₂₁FN₂O
Molecular Weight:
405.35
Synonyms:
1-(3-Dimethylaminopropyl)-1-(4-fluorophenyl)-5-cyanophthalan;1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile;Bonitrile;Lu 10-171;Nitalapram;
EINECS:
261-891-1
Density:
1.18 g/cm³
Melting Point:
182-183 °C
Boiling Point:
428.3 °C at 760 mmHg
Flash Point:
212.8 °C
Appearance:
grease
Transport Information:
UN 3249

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Reference

Antagonism of fenfluramine-induced hyperthermia in rats by some, but not all, selective inhibitors of 5-hydroxytryptamine uptake: Antagonism of fenfluramine-induced hyperthermia in rats by some, but not all, selective inhibitors of 5-hydroxytryptamine uptake. Sugrue, M. F. (Cent. Rech., Merrell Int., Strasbourg, Fr.). Br. J. Pharmacol., 81(4), 651-7 (English) 1984. CODEN: BJPCBM. ISSN: 0007-1188. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The injection of fenfluramine [458-24-2] (7.5 mg/kg, i.p.) to rats housed at 27-28° was assocd. with an elevation of core body temp. which peaked at approx. 1 h post-injection. One h pretreatment with citalopram [59729-33-8] (20 mg/kg, i.p.), chlorimipramine [303-49-1] (10 mg/kg, i.p.), femoxetine [59859-58-4] (10 mg/kg, i.p.), and fluoxetine [54910-89-3] (20 mg/kg, i.p.) resulted in an attenuated response to fenfluramine. In contrast, Org 6582 [59905-71-4] (20 mg/kg) and zimelidine [56775-88-3] (20 mg/kg) were devoid of an effect on fenfluramine-induced hyperthermia. The response to fenfluramine was also blocked by i.p. injections of metergoline [17692-51-2] (0.2 mg/kg), methylsergide [361-37-5] (5 mg/kg) and mianserin [24219-97-4] (0.5 mg/kg). Rectal temp. was unaltered by both the 5-HT [50-67-9] uptake inhibitors and the 5-HT receptor antagonists. The IC50 values (nM) for in vitro inhibition of [3H]-5-HT uptake into rat hypothalamic synaptosomes were for citalopram 2.4, chlorimipramine 8. 24219-97-4 and 50-67-9 are cas registry numbers of chemicals which are used as reagents here.8, femoxetine 14, fluoxetine 16, Org 6582 75 and zimelidine 250. The injection of all 6 compds. (20 mg/kg, i.p.) 1 h before death was assocd. with an inhibition of [3H]-5-HT uptake into rat hypothalamic synaptosomes which ranged from 47.2% for chlorimipramine to 83.3% for citalopram. Rat hypothalamic 5-HT levels were decreased by approx. 50% 3 h after the injection of fenfluoramine (15 mg/kg, i.p.). This effect was blocked by a 1 h pretreatment with fluoxetine, Org 6582 and zimelidine (all 20 mg/kg, i.p.). Ki Values for displacement of specifically bound [3H]-5-HT (1 nM) to rat hypothalamic membranes were for metergoline 26 nM, methysergide 1.1 mM, mianserin 3.6 mM, chlorimipramine 9.2 mM and fluoxetine 32.7 mM. Values for citalopram, femoxetine, Org 6582 and zimelidine were in excess of 65.4 mM. Fenfluoramine-induced hyperthermia in rats was blocked by citalopram, chlorimipramine, femoxetine, and fluoxetine but not by Org 6582 and zimelidine. This dichotomy cannot be explained in terms of differences in 5-HT uptake, storage and release mechanisms in the rat hypothalamus. Moreover, antagonism of fenfluramine-induced hyperthermia cannot be attributed to blockade of central, postsynaptic 5-HT receptors. The involvement of an indoleamine other than 5-HT is discussed. .

Comparative animal studies on cardiovascular toxicity of tri- and tetracyclic antidepressants and citalopram; relation to drug plasma levels: Comparative animal studies on cardiovascular toxicity of tri- and tetracyclic antidepressants and citalopram; relation to drug plasma levels. Boeck, V.; Joergensen, A.; Fredricson Overoe, K.In this study， 72-69-5 and 1668-19-5 are also used. (Res. Lab., H. Lundbeck and Co., Copenhagen-Valby DK-2500, Den.). Psychopharmacology (Berlin), 82(4), 275-81 (English) 1984. CODEN: PSCHDL. ISSN: 0033-3158. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The cardiovascular and(or) cardiotoxic effects of 8 antidepressants (imipramine [50-49-7], chlorimipramine [303-49-1], amitriptyline [50-48-6], nortriptyline [72-69-5], doxepin [1668-19-5], maprotiline [10262-69-8], mianserin [24219-97-4], and citalopram [59729-33-8]) were compared in anesthetized cats after oral dosing and in conscious rabbits after i.v. infusion. In cats, drug plasma levels were detd. as well. Citalopram and chlorimipramine in particular, but also mianserin, appeared less cardiotoxic than the other drugs tested. The cardiovascular effects seen in the cats were with few exceptions identical for all the drugs tested but not seen at the same dose. Safety margins were defined as minimal doses or plasma levels when ECG changes (conduction or rhythm) or cardiovascular effects (±10% change of initial value in a series of parameters) occurred in exptl. animals divided by maximal therapeutic dose or mean plasma levels in patients. Except for citalopram and mianserin (safety margins 80 and 18 resp. in cats and > 15 in rabbits), all the other drugs tested (safety margins ￡9) have a cardiotoxic potential. The probability that the cardiovascular side effects may occur is less pronounced for citalopram (safety margins 10-32) than for all the other drugs tested (safety margins ranging from 0.1 to <5). .

Detail of "59729-33-8"

5-Isobenzofurancarbonitrile,1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-

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CAS No.59729-33-8 Citalopram

CAS No.59729-33-8 Citalopram

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CAS No.59729-33-8 Citalopram

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CAS No.59729-33-8 Citalopram

Reference