Reference

Neurochemical characterization of a new potent and selective serotonin uptake inhibitor: Lu 10-171

Neurochemical characterization of a new potent and selective serotonin uptake inhibitor: Lu 10-171. Hyttel, John (Dep. Pharmacol. Toxicol., H. Lundbeck and Co. A/S, Copenhagen-Valby, Den.). Psychopharmacology (Berlin), 51(3), 225-33 (English) 1977. CODEN: PSCHDL. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) The neurochem. characteristics of a new bicyclic phthalane deriv., Lu 10-171-HBr (citalopram-HBr)(I) [59729-32-7] were investigated. I and its metabolites were compared with tricyclic thymoleptics in several tests for serotonin (5-HT) [50-67-9], noradrenaline (NA), and dopamine (DA) uptake inhibition in vitro and in vivo. I was a very potent and completely selective inhibitor of the 5-HT reuptake mechanism, being 2-10 times as active as chlorimipramine. The metabolites of I showed weak 5-HT uptake inhibiting properties. I and its metabolites were devoid of NA uptake inhibiting properties and in this respect they clearly differ from the tricyclic antidepressants, which possess effects both on 5-HT and NA uptake. The inhibition of 5-HT uptake in vitro was competitive and not connected with an increased efflux of 5-HT. I and its metabolites only inhibited DA uptake in extremely high concns. and in this respect they were even weaker than chlorimipramine and other tricyclic thymoleptics. Like the tricyclic thymoleptics, I was without effect on MAO and did not change the endogenous levels of brain monoamines. Due to the selective action on 5-HT uptake, I seems to be a valuable tool in studying the role of central 5-HT neurone systems in exptl. neuropharmacol. as well as in the etiol. of depressive illness.Except for chemicals metioned above, 62498-71-9 and 62498-70-8 are also used. .

A pharmaceutical dosage form of citalopram

A pharmaceutical dosage form of citalopram. Dabre, Rahul; Singla, Ajay Kumar; Sethi, Sanjeev; Malik, Rajiv ( Ranbaxy Laboratories Limited, India). PCT Int. Appl. WO 2004103361 A2 2 Dec 2004, 16 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization).Some commonly used reagents like 59729-32-7 and 59729-33-8 are used in this experiment. CODEN: PIXXD2. CLASS: ICM: A61K031-343. APPLICATION: WO 2004-IB1657 21 May 2004. PRIORITY: IN 2003-DE712 20 May 2003; IN 2003-DE710 20 May 2003. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 The present invention relates to pharmaceutical dosage forms of citalopram and processes of prepn. thereof. About 36% of the citalopram particles, by vol., have a particle size that is <5 mm. The citalopram particles may have an av. aspect ratio of <2. Thus, tablets contained micronized citalopram-HBr 50.0, microcryst. cellulose 25.0, lactose monohydrate 80.0, starch 70.0, Croscarmellose sodium 5.0, and crosslinked PVP 9.0 mg/tablet and water qs. .