serotonin transporter ( Ki = 0.89 nM ); DAT ( Ki = 10500 nM ); NET ( Ki = 8150 nM )

体外活性：艾司西酞普兰是西酞普兰的 S-对映体，属于一类被称为选择性血清素再摄取抑制剂 (SSRI) 的抗抑郁药。它用于治疗与情绪障碍相关的抑郁症。它偶尔也用于治疗身体变形障碍和焦虑。据推测，艾司西酞普兰的抗抑郁、抗强迫症和抗贪食作用与其抑制中枢神经系统神经元摄取血清素有关。体外研究表明，艾司西酞普兰是神经元血清素再摄取的有效且选择性抑制剂，并且对去甲肾上腺素和多巴胺神经元再摄取仅具有非常微弱的作用。艾司西酞普兰对肾上腺素能（α1、α2、β）、胆碱能、GABA、多巴胺能、组胺能、血清素能（5HT1A、5HT1B、5HT2）或苯二氮卓受体没有显着的亲和力；据推测，此类受体的拮抗作用与其他精神药物的各种抗胆碱能、镇静和心血管作用有关。研究发现，长期服用艾司西酞普兰会下调大脑去甲肾上腺素受体，正如在其他有效治疗重度抑郁症的药物中观察到的那样。艾司西酞普兰不抑制单胺氧化酶。

Male Sprague-Dawley rats
10 mg/kg
I.p.; daily for 28 days

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Escitalopram is the active S-isomer of the antidepressant, citalopram. Limited information indicates that maternal doses of escitalopram up to 20 mg daily produce low levels in milk and would not be expected to cause any adverse effects in breastfed infants, especially if the infant is older than 2 months. If escitalopram is required by the mother, it is not a reason to discontinue breastfeeding. A safety scoring system finds escitalopram use to be possible during breastfeeding. One case of necrotizing enterocolitis was reported in a breastfed newborn whose mother was taking escitalopram during pregnancy and lactation, but causality was not established. A seizure-like event occurred in an infant who was also exposed to bupropion in milk. Other minor behavioral problems have also been reported. Monitor the infant for excess drowsiness, restlessness, agitation, poor feeding and poor weight gain, especially in younger, exclusively breastfed infants and when using combinations of psychotropic drugs.
Mothers taking a selective serotonin reuptake inhibitor (SSRI) like escitalopram during pregnancy and postpartum may have more difficulty breastfeeding, although this might be a reflection of their disease state. These mothers may need additional breastfeeding support. Infants exposed to an SSRI during the third trimester of pregnancy have a lower risk of poor neonatal adaptation if they are breastfed than formula-fed infants.
◉ Effects in Breastfed Infants
Eight breastfed infants whose mothers were taking escitalopram in an average dose of 199 mcg/kg daily for postpartum depression were evaluated by a pediatric specialist using the Denver developmental scale. Their mothers had taken escitalopram for a median of 55 days postpartum (range 23 to 240 days). The infants' scores on this scale was 110% of normal.
A woman began taking escitalopram 5 mg daily immediately after birth. Her dosage was increased to 10 mg daily and valproic acid 1200 mg daily was added by 7 weeks postpartum. Her breastfed infant was judged to be healthy and have normal neuropsychological development by a general practitioner at 7.5 weeks of age.
One woman was taking escitalopram 20 mg daily and reboxetine 4 mg daily orally while nursing her infant (extent not stated). She had taken reboxetine for 1.5 months, but the start of her escitalopram therapy was not stated. At 9.5 months of age, her breastfed infant had normal weight gain and a Denver developmental score of 105% of chronological age.
A nursing mother was given escitalopram 10 mg daily for depression beginning at 3 weeks postpartum and increasing to 20 mg daily thereafter. At 4 months of age, her exclusively breastfed infant was admitted to the hospital for irritability, vomiting and fever of 4 days duration. He had been irritable with prolonged periods of crying for the past 3 months according to his mother and had gained only 400 grams per month since birth. Liver enzymes were moderately elevated. The infant was discharged after 5 days and breastfeeding was continued, but only twice daily for 2 weeks, then discontinued at 4.5 months of age. At 5 months, symptom improvement was noted and at 6 months, serum liver enzymes had normalized. The author noted that the time course of the adverse effects were consistent with the treatment with escitalopram.
A mother began taking escitalopram 20 mg daily in the morning on day 15 postpartum. She exclusively breastfed her infant on demand. At 3 months of age, no adverse effects had been reported in the infant by his pediatrician.
At 5 days of age, an infant was readmitted to the neonatal intensive care unit with a diagnosis of necrotizing enterocolitis. The infant had spent the first 2 days of life in intensive care because of respiratory distress. The infant's mother had taken escitalopram 20 mg daily throughout pregnancy and while breastfeeding (extent not stated). The authors hypothesized that escitalopram might have been responsible for the enterocolitis because of its effect on platelet aggregation. The drug was possibly a cause of the reaction.
One author reported on the newborn infant of a mother who was taking escitalopram (dose and duration not stated). The hyperirritable infant had high-pitched crying 2 hours after breastfeeding every afternoon which was 5 to 6 hours after maternal dose of escitalopram. Changing the time of the mother's escitalopram dose resulted in a shift in the time of the infant's crying at the same time interval after the dose. The infant's symptoms improved with partial substitution of formula and ceased on day 11 of life with complete formula feeding.
An uncontrolled online survey compiled data on 930 mothers who nursed their infants while taking an antidepressant. Infant drug discontinuation symptoms (e.g., irritability, low body temperature, uncontrollable crying, eating and sleeping disorders) were reported in about 10% of infants. Mothers who took antidepressants only during breastfeeding were much less likely to notice symptoms of drug discontinuation in their infants than those who took the drug in pregnancy and lactation.
A 6.5-month-old infant developed severe vomiting and an apparent tonic seizure after being breastfed by her mother. The mother had been taking escitalopram 10 mg daily since birth and had begun extended-release bupropion 150 mg daily 3 weeks earlier. The seizure occurred 8 hours after the mother's morning dose of bupropion. The infant's mother had noted disturbances in sleep behavior, unusual movements, and unresponsiveness followed by sleep on several previous occasions. The baby was partially breastfed, also receiving pumped breastmilk, formula, and solid foods. Breastfeeding was discontinued and the baby was discharged after being asymptomatic for 48 hours. The seizure was probably drug-related, most likely caused by bupropion and hydroxybupropion in breastmilk, but a contribution by escitalopram cannot be ruled out.
A cohort of 247 infants exposed to an antidepressant in utero during the third trimester of pregnancy were assessed for poor neonatal adaptation (PNA). Of the 247 infants, 154 developed PNA. Infants who were exclusively given formula had about 3 times the risk of developing PNA as those who were exclusively or partially breastfed. None of the infants were exposed to escitalopram in utero, but 51 were exposed to citalopram, the racemic form of the drug.
A case-control study in Israel compared 280 infants of nursing mothers taking long-term psychotropic drugs to the infants of 152 women taking antibiotics. Infant sleepiness at 3 days of age was reported by 3 mothers taking escitalopram during pregnancy and breastfeeding and by none taking antibiotics. The sleepiness resolved within 24 hours with no developmental effect.
A mother with mixed anxiety-depressive order was taking sertraline and breastfeeding her 9-month-old infant. Because of side effects, sertraline was stopped and citalopram 10 daily was started. After 2 weeks of therapy, she reported signs of bruxism in her infant who was breastfed 5 to 6 times daily, as well as supplementary feedings such as fruits, vegetables, meat, and biscuits. The infant had sporadic, pulsatile, and momentary movements in her jaws, which usually began with movements of the head, especially during sleep. Furthermore, the mother mentioned her child had a habit of biting and clenching her teeth while awake. Pediatric and dental examinations found no abnormalities, but the dentist observed bruxism during the examination. Citalopram was discontinued and bruxism symptoms resolved after 72 hours. The mother resumed breastfeeding with no return of symptoms and the infant had no bruxism symptoms for the next 2 years. Bruxism was probably caused by citalopram in breastmilk.
◉ Effects on Lactation and Breastmilk
The SSRI class of drugs, including escitalopram, can cause increased prolactin levels and galactorrhea in nonpregnant, nonnursing patients. Euprolactinemic galactorrhea has also been reported. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.
In a small prospective study, 8 primiparous women who were taking a serotonin reuptake inhibitor (SRI; 3 taking fluoxetine and 1 each taking citalopram, duloxetine, escitalopram, paroxetine or sertraline) were compared to 423 mothers who were not taking an SRI. Mothers taking an SRI had an onset of milk secretory activation (lactogenesis II) that was delayed by an average of 16.7 hours compared to controls (85.8 hours postpartum in the SRI-treated mothers and 69.1 h in the untreated mothers), which doubled the risk of delayed feeding behavior in the untreated group. However, the delay in lactogenesis II may not be clinically important, since there was no statistically significant difference between the groups in the percentage of mothers experiencing feeding difficulties after day 4 postpartum.
A case control study compared the rate of predominant breastfeeding at 2 weeks postpartum in mothers who took an SSRI antidepressant throughout pregnancy and at delivery (n = 167) or an SSRI during pregnancy only (n = 117) to a control group of mothers who took no antidepressants (n = 182). Among the two groups who had taken an SSRI, 33 took citalopram, 18 took escitalopram, 63 took fluoxetine, 2 took fluvoxamine, 78 took paroxetine, and 87 took sertraline. Among the women who took an SSRI, the breastfeeding rate at 2 weeks postpartum was 27% to 33% lower than mother who did not take antidepressants, with no statistical difference in breastfeeding rates between the SSRI-exposed groups.
An observational study looked at outcomes of 2859 women who took an antidepressant during the 2 years prior to pregnancy. Compared to women who did not take an antidepressant during pregnancy, mothers who took an antidepressant during all 3 trimesters of pregnancy were 37% less likely to be breastfeeding upon hospital discharge. Mothers who took an antidepressant only during the third trimester were 75% less likely to be breastfeeding at discharge. Those who took an antidepressant only during the first and second trimesters did not have a reduced likelihood of breastfeeding at discharge. The antidepressants used by the mothers were not specified.
A retrospective cohort study of hospital electronic medical records from 2001 to 2008 compared women who had been dispensed an antidepressant during late gestation (n = 575) to those who had a psychiatric illness but did not receive an antidepressant (n = 1552) and mothers who did not have a psychiatric diagnosis (n = 30,535). Women who received an antidepressant were 37% less likely to be breastfeeding at discharge than women without a psychiatric diagnosis, but no less likely to be breastfeeding than untreated mothers with a psychiatric diagnosis. None of the mothers were taking escitalopram.
In a study of 80,882 Norwegian mother-infant pairs from 1999 to 2008, new postpartum antidepressant use was reported by 392 women and 201 reported that they continued antidepressants from pregnancy. Compared with the unexposed comparison group, late pregnancy antidepressant use was associated with a 7% reduced likelihood of breastfeeding initiation, but with no effect on breastfeeding duration or exclusivity. Compared with the unexposed comparison group, new or restarted antidepressant use was associated with a 63% reduced likelihood of predominant, and a 51% reduced likelihood of any breastfeeding at 6 months, as well as a 2.6-fold increased risk of abrupt breastfeeding discontinuation. Specific antidepressants were not mentioned.

[1]. Encephale . 2007 Dec;33(6):965-72.

[2]. J Med Chem . 2010 Aug 26;53(16):6112-21.

Escitalopram Oxalate is the oxalate salt of escitalopram, a pure S-enantiomer of the racemic bicyclic phthalane derivative citalopram, with antidepressant activity. As a selective serotonin reuptake inhibitor (SSRI), escitalopram blocks the reuptake of serotonin by neurons in the central nervous system (CNS), thereby potentiating CNS serotonergic activity.
S-enantiomer of CITALOPRAM. Belongs to a class of drugs known as SELECTIVE SEROTONIN REUPTAKE INHIBITORS, used to treat depression and generalized anxiety disorder.
See also: Escitalopram (has active moiety).

C22H23FN2O5

414.43

414.159

C, 63.76; H, 5.59; F, 4.58; N, 6.76; O, 19.30

219861-08-2

Escitalopram; 128196-01-0; Escitalopram-d6 oxalate; 1217733-09-9; Escitalopram-d4 oxalate

146571

White to off-white solid powder

428.3ºC at 760 mmHg

152-153ºC

212.8ºC

2.968

110.86

2

8

6

30

537

1

FC1C([H])=C([H])C(=C([H])C=1[H])[C@]1(C2C([H])=C([H])C(C#N)=C([H])C=2C([H])([H])O1)C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])[H].O([H])C(C(=O)O[H])=O

KTGRHKOEFSJQNS-BDQAORGHSA-N

InChI=1S/C20H21FN2O.C2H2O4/c1-23(2)11-3-10-20(17-5-7-18(21)8-6-17)19-9-4-15(13-22)12-16(19)14-24-20;3-1(4)2(5)6/h4-9,12H,3,10-11,14H2,1-2H3;(H,3,4)(H,5,6)/t20-;/m0./s1

(1S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-3H-2-benzofuran-5-carbonitrile;oxalic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 请将本产品存放在密封且受保护的环境中，避免吸湿/受潮。

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

配方 1 中的溶解度: ≥ 100 mg/mL (241.30 mM) (饱和度未知) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。