Panamesine
(Synonyms: EMD 57445) 目录号 : GC61926
Panamesine (EMD 57445) 是一种高亲和力的 sigma 受体配体，IC50 为 6 nM，有潜力用于非典型抗精神病的研究。
Cas No.:139225-22-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >99.50%
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- Datasheet
Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent[1].
Panamesine (EMD 57445; 0.3, 1, 3, 30 mg/kg) induces a dose-dependent increase of c-fos expression in several cortical areas with the strongest signals in the piriform cortex[1].
References:
[1]. N Dahmen, et al. Induction of C-Fos Gene Expression by the Selective Sigma Receptor Ligand EMD 57445 in Rat Brain. Eur Neuropsychopharmacol. 1996 Aug;6(3):237-43.
| Cas No. | 139225-22-2 | SDF | |
| 别名 | EMD 57445 | ||
| Canonical SMILES | O=C1O[C@@H](CN2CCC(O)(C3=CC=C(OCO4)C4=C3)CC2)CN1C5=CC=C(OC)C=C5 | ||
| 分子式 | C23H26N2O6 | 分子量 | 426.46 |
| 溶解度 | DMSO : 125 mg/mL (293.11 mM) | 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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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3449 mL | 11.7244 mL | 23.4489 mL |
| 5 mM | 0.469 mL | 2.3449 mL | 4.6898 mL |
| 10 mM | 0.2345 mL | 1.1724 mL | 2.3449 mL |
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动物数量 | 只 |
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2.
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Characterization of the sigma ligand Panamesine, a potential antipsychotic, by immune response in patients with schizophrenia and by sleep-EEG changes in normal controls
Psychopharmacology (Berl) 1999 Jan;141(1):107-10.PMID:9952072DOI:10.1007/s002130050813.
Panamesine (PAN) is a nearly specific sigma ligand. Recently, we showed that PAN in doses up to 90 mg/day improved psychometric variables in patients with an acute episode of schizophrenia. No side effects connected to the extrapyramidal motoric system occurred; there was even an absence of daytime sedation. We investigated the effects of PAN on plasma cytokine and soluble cytokine receptor levels and blood cell counts during 4 weeks in ten patients out of the previous study sample. Under PAN treatment, tumor necrosis factor (TNF)-alpha, soluble TNF receptors p55 and p75, and soluble interleukin-2 receptor levels were not increased and neither were monocyte and lymphocyte counts affected. This absence of immunomodulation is in contrast to clozapine, but similar to haloperidol treatment. In a second study, a single dose of PAN (30 mg) or placebo was administered at 2200 hours to ten young male controls in order to investigate changes in the sleep EEG under the substance. Sleep efficiency index increased, whereas time spent awake decreased. No significant changes in rapid eye movement (REM) sleep or non-REM parameters occurred. The sleep-EEG investigation showed sleep-consolidating effects of the drug, comparable to those of classical neuroleptics. Our results support the hypothesis that the sigma ligand PAN, which has antipsychotic properties, shares biological aspects with haloperidol.
Open clinical trial on the sigma ligand Panamesine in patients with schizophrenia
Psychopharmacology (Berl) 1997 Jul;132(1):82-8.PMID:9272763DOI:10.1007/s002130050323.
The sigma (sigma) receptor has been proposed as a target of neuroleptic drugs. Preclinical data suggest that Panamesine (EMD 57445), a novel sigma ligand, has antipsychotic effects and is free of side effects related to the extrapyramidal motoric system (EPMS). Here we report the results of an exploratory study aimed at determining the appropriate dose range and the safety of Panamesine in patients with an acute episode of schizophrenia. The first trial with four patients revealed insufficient clinical efficacy of a protocol where the daily dosage was increased stepwise from 7.5 mg during week 1, up to 30 mg during weeks 3 and 4. In a second set of trials, 12 patients received 15 mg at the beginning, this being increased up to 60 mg/day within 3 days and then maintained at this level for 4 weeks. As assessed by a decrease in the Brief Psychiatric Rating Scale score by at least 50%, five patients were judged as responders, whereas six patients showed only a slight improvement, and one deteriorated. Moreover, intent-to-treat analysis showed significant improvement in psychometric variables. In all patients prolactin levels increased during treatment, probably due to an active metabolite with weak dopamine-2-receptor antagonistic effects. No major side effects occurred, and in particular, no EPMS symptoms were seen.
[Atypical antipsychotic profiles of sigma receptor ligands]
Nihon Yakurigaku Zasshi 1999 Jul;114(1):13-23.PMID:10562961DOI:10.1254/fpj.114.13.
This is a review on the recent results of research on sigma-receptor antagonists. NE-100, a selective sigma1-receptor antagonist, shows improvement of abnormal behaviors and cognitive dysfunction induced by phencyclidine (PCP). However, NE-100 does not inhibit dopamine agonist-induced behaviors nor induces catalepsy. The mode of action of NE-100 is estimated to be the indirect modulation of the NMDA/PCP-receptor ion channel complex and the modulation of dopamine release from the dopaminergic nerve terminals. The recently reported MS-355/MS-377, which is also a selective sigma1-receptor antagonist, has a similar pharmacological profiles as NE-100, but in addition, MS-355/MS-377 inhibits methamphetamine-induced formation of reversal tolerance and also inhibits apomorphine-induced climbing behavior like dopamine D2-receptor antagonists. The report on clinical trial targeting schizophrenia shows results on rimcazole, remoxipride, BMY 14802, Panamesine (EMD 57445) and SL 82.0715. Rimcazole was effective in the open study, but the double blind trial was discontinued due to seizure induction. Remoxipride showed efficacy different from those of dopamine D2-receptor antagonists (less extrapyramidal adverse effects), but the trial was discontinued due to occurrence of aplastic anemia. Panamesine and SL 82.0714 showed favorable efficacy in the open studies, but BMY 14802 showed no efficacy in clinical trials.
Antipsychotic effects and tolerability of the sigma ligand EMD 57445 (Panamesine) and its metabolites in acute schizophrenia: an open clinical trial
Psychiatry Res 1999 Dec 27;89(3):275-80.PMID:10708274DOI:10.1016/s0165-1781(99)00100-6.
Antipsychotic efficacy and side effects of the selective sigma ligand EMD 57445 (Panamesine) were investigated in 12 patients (6 males, 6 females) who met DSM-III-R criteria for schizophrenia. A 4-week open clinical study revealed only modest effects of EMD 57445 and its metabolites on positive and negative symptoms of schizophrenia. Extrapyramidal and other side effects were moderate, although a significant increase in mild dyskinetic movements was found. Five patients, four of whom were females, completed the trial. Dropouts were mainly due to treatment failure. Antipsychotic effects were significantly greater in female than male patients.
Efficacy and safety of the sigma receptor ligand EMD 57445 (Panamesine) in patients with schizophrenia: an open clinical trial
Pharmacopsychiatry 1999 Mar;32(2):68-72.PMID:10333165DOI:10.1055/s-2007-979194.
EMD 57455 (Panamesine) is a new sigma receptor ligand alleged to have antipsychotic effects. Animal studies have demonstrated that EMD 57445 has a functional antidopaminergic activity without extrapyramidal side effects and a c-fos expression pattern similar to that obtained with atypical neuroleptics. Therefore, the substance might be of interest for the treatment of schizophrenia. The present article describes the results of an exploratory open clinical trial that was aimed at determining the appropriate dose range for clinical efficacy and safety of EMD 57455 in patients with an acute episode of schizophrenia. In a treatment period of 4 weeks, 12 patients received EMD 57445 up to 60 mg/day for 4 weeks. Seven patients completed the study: four were classified as responders (as defined by at least a 50% decrease in the BPRS total score), two improved slightly and one patient remained unimproved. The intent-to-treat analysis showed significant improvement in the psychometric variables assessed by the Brief Psychiatric Rating Scale, Clinical Global Impression and Positive and Negative Symptoms Scale. Major side effects were extrapyramidal symptoms in two patients and restlessness in one patient. With respect to efficacy and safety, our data agree with a previous study, except that in our study EMD 57455 was not totally free of extrapyramidal side effects.