Clocapramine (Clocarpramine)
(Synonyms: Clocarpramine; 3-Chlorocarpipramine) 目录号 : GC31037
Clocapramine是多巴胺D2和5-HT2A受体拮抗剂。
Cas No.:47739-98-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats[2] Male Wistar rats (210 to 240 g) are housed in a temperature-controlled room with a 12-hour dark/light cycle (lights on at 8:30) and have free access to food and water. For competition studies, rats are pretreated with an intraperitoneal injection of varying doses of antipsychotic drugs or the same volume (0.21 to 0.24 mL) of the corresponding vehicle (DMSO), 10 minutes prior to the injection of [3H]-YM-09151-2 or [3H]-ketanserin. |
References: [1]. Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. | |
Clocapramine is an antagonist of the D2, 5-HT2A receptors.
Clocapramine has a moderate affinity for D2-receptors in vitro. Clocapramine shows higher affinity for 5-HT2A than for D2-receptors in vitro[1].
Clocapramine shows the lowest potency for D2-occupancy in vivo[1]. An in vivo receptor binding technique is used to evaluate the binding profiles of typical and atypical antipsychotic drugs to striatal dopamine-D2 and frontal serotonin-5-HT2 receptors in a rat brain using more specific ligands. Clocapramine produces ratios of potency in occupying 5-HT2 versus D2 receptors that fall between these two groups (ED50 of 14.5 mg/kg for D2, 4.9 mg/kg for 5-HT2)[2].
[1]. Schotte A, et al. In vitro receptor binding and in vivo receptor occupancy in rat and guinea pig brain: risperidone compared with antipsychotics hitherto used. Jpn J Pharmacol. 1995 Dec;69(4):399-412. [2]. Sumiyoshi T, et al. Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy. Neuropsychopharmacology. 1995 Feb;12(1):57-64.
| Cas No. | 47739-98-0 | SDF | |
| 别名 | Clocarpramine; 3-Chlorocarpipramine | ||
| Canonical SMILES | O=C(C1(N2CCCCC2)CCN(CCCN3C4=CC(Cl)=CC=C4CCC5=CC=CC=C53)CC1)N | ||
| 分子式 | C28H37ClN4O | 分子量 | 481.07 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0787 mL | 10.3935 mL | 20.787 mL |
| 5 mM | 0.4157 mL | 2.0787 mL | 4.1574 mL |
| 10 mM | 0.2079 mL | 1.0393 mL | 2.0787 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Efficacy and safety of antipsychotic treatments for schizophrenia: A systematic review and network meta-analysis of randomized trials in Japan
Background: We examined the efficacy and safety of using antipsychotic medication for schizophrenia using only randomized trials of antipsychotic for schizophrenia conducted in Japan to avoid the biological and environmental heterogeneities caused by pooling data from various races and ethnicities. Methods: We searched for eligible studies on Embase, PubMed, and CENTRAL. Primary outcomes were improvement in Positive and Negative Syndrome Scale total score (PANSS-T) and all-cause discontinuation. Other outcomes were improvement in PANSS subscale scores, discontinuation due to adverse events or inefficacy, and the incidence of 16 adverse events. Results: We calculated mean difference or risk ratios and 95% credible intervals. We identified 34 RCTs (6798 patients; mean study duration, 9.0 ± 4.24 weeks; proportion of male patients, 53.7%; mean age, 43.3 years). Besides placebo, studies included aripiprazole, asenapine, blonanserin, blonanserin-patch, brexpiprazole, clocapramine (no PANSS data), clozapine (no PANSS data), haloperidol, lurasidone, mosapramine, olanzapine, paliperidone, perospirone, quetiapine, and risperidone. Efficacy and safety profiles differed for antipsychotics used with schizophrenia in Japanese patients. All active treatments other than haloperidol and quetiapine outperformed placebo to improve PANSS-T. Asenapine, olanzapine, paliperidone, and risperidone outperformed placebo for all-cause discontinuation. Asenapine, blonanserin, blonanserin-patch, haloperidol, lurasidone, mosapramine, olanzapine, paliperidone, and risperidone outperformed placebo to improve PANSS positive subscale scores. Aripiprazole, asenapine, blonanserin, blonanserin-patch, brexpiprazole, lurasidone, olanzapine, paliperidone, perospirone, and risperidone outperformed placebo to improve PANSS negative subscale scores. The confidence in evidence of most outcomes was low or very low. Conclusion: Our results are similar to those of previous network meta-analysis involving various races and ethnicities.
Iminodibenzyl class antipsychotics for schizophrenia: a systematic review and meta-analysis of carpipramine, clocapramine, and mosapramine
Background: We conducted a meta-analysis of the iminodibenzyl antipsychotics carpipramine, clocapramine, and mosapramine, which are classified as second-generation antipsychotics (SGAs) for schizophrenia treatment.
Methods: We searched data that had been published in PubMed, the Cochrane Library databases, PsycINFO, CiNii, and the Japan Medical Abstracts Society up to August 29, 2014. Randomized controlled trials that compared iminodibenzyl antipsychotics with other antipsychotics in patients with schizophrenia were included. Odds ratios and standardized mean differences were evaluated.
Results: We included four randomized controlled trials on carpipramine (number of patients [n]=290), six on clocapramine (n=1,048), and five on mosapramine (n=986) in the meta-analysis. There were no significant differences in the response rates or in the discontinuation rates either between carpipramine and the other pooled antipsychotics or between clocapramine and the other pooled antipsychotics. On the Positive and Negative Syndrome Scale, mosapramine's positive subscale scores were superior to those of the other pooled antipsychotics (standard mean of difference =-0.22); however, on that same scale, there were no significant differences in total scores, negative scores, general subscale scores, response rates, or the discontinuation rates between mosapramine and the other pooled antipsychotics. Furthermore, the incidences of extrapyramidal symptoms and of hyperprolactinemia were significantly greater with mosapramine than with the other pooled antipsychotics.
Conclusion: The pharmacological profiles of carpipramine and clocapramine, which are classified as SGAs, were similar to those of first-generation antipsychotics because there were no significant differences in efficacy and safety outcomes. However, mosapramine was associated with a greater risk of extrapyramidal symptoms and hyperprolactinemia than the other SGAs were, although it may be beneficial for the improvement of positive symptoms.
A crossover study of clocapramine and haloperidol in chronic schizophrenia
Therapeutic efficacy and target symptoms with clocapramine were compared with those with haloperidol by the crossover method, in a total of 26 chronic schizophrenic patients, by administration of one of the drugs for the first 14 weeks and the other for the next 14 weeks. The final global improvement rating showed no significant difference between the two groups, but clocapramine administered as first drug appeared to have a more pronounced effect than haloperidol. According to the improvement rate in psychotic symptoms, clocapramine tended to be superior to haloperidol for motor retardation, scanty speech and disturbance of thought. In addition the frequency of side-effects was lower with clocapramine than with haloperidol. Neither the side-effects nor abnormal laboratory test results were severe enough to terminate the trial. Clocapramine is considered to be equivalent or superior to haloperidol in terms of anti-psychotic effect in chronic schizophrenia, and is relatively safer than haloperidol.
A single-blind study of clocapramine and sulpiride in hospitalized chronic schizophrenic patients
The therapeutic effects, safety and side-effects of clocapramine and sulpiride were evaluated in 52 hospitalized chronic schizophrenic patients using a single-blind method during an 8-week trial period. While the final global improvement rating showed clocapramine to be superior to sulpiride, the differences were not statistically significant. The time course of the total psychiatric rating scales (PRS) showed a progressive decline during treatment for both drugs, and at the end of treatment clocapramine proved significantly lower in total PRS than did sulpiride. In the improvement of psychotic symptoms, clocapramine seemed to be superior to sulpiride with respect to motor retardation, delusion, hallucination or disturbance of self-consciousness, social isolation or withdrawal, and recreation or work. Side-effects appeared more frequently with clocapramine than with sulpiride, but abnormal laboratory-test results appeared less in clocapramine-treated patients than in sulpiride-treated ones. Neither side-effects nor abnormal laboratory-test results induced by the two drugs were severe enough to terminate administration. Clocapramine is concluded to have a more favourable effect on negative symptoms, as well as on some positive symptoms of chronic schizophrenia, than sulpiride.
Pharmacokinetic study of iminodibenzyl antipsychotic drugs, clocapramine and Y-516 in dog and man
The pharmacokinetic properties of the iminodibenzyl antipsychotic drugs clocapramine (CCP, 3-chloro-5-[3-(4-carbamoyl-4-piperidino piperidino) propyl]-10, 11-dihydro-5H-dibenzo[b, f]azepine) and Y-516 (3-chloro-5-[3-(2-oxo-1, 2, 3, 5, 6, 7, 8, 8a-octahydroimidazo [1,2-a] pyridine-3-spiro-4'-piperidino) propyl]-10, 11-dihydro-5H-dibenzo[b, f]azepine) were investigated in dog and man. Dogs were administered CCP and Y-516 intravenously, intraperitoneally, and orally, and the concentrations of the parent drugs and their metabolites in the plasma and urine were determined. Half-life (t1/2) was approximately the same by all three administration routes, being approximately 5 h for CCP and 3 h for Y-516. Bioavailability following oral administration was 0.16 +/- 0.01 (mean +/- SD, n = 3) for CCP and 0.29 +/- 0.07 for Y-516. The fractions of dose absorbed following oral administration were 0.43 +/- 0.07 and 0.79 +/- 0.24, and the fractions of dose metabolized in the liver due to the first-pass effect were 0.63 +/- 0.05 and 0.63 +/- 0.04 for CCP and Y-516, respectively. Y-516 was detected in the plasma after intraperitoneal and oral administration of CCP. The ratio of the AUC of Y-516 to that of CCP was 0.06 following intraperitoneal administration and 0.40 following oral administration. This indicated that while the metabolism of CCP into Y-516 may occur partly in the liver due to the first-pass effect, it occurs mostly within the gastrointestinal tract itself or its mucosa.(ABSTRACT TRUNCATED AT 250 WORDS)