2-Methyl-5-HT
(Synonyms: 2-甲基-5-羟基色氨酸盐酸,2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT) 目录号 : GC38108
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) 是一种有效的选择性 5-HT3 受体激动剂。2-Methyl-5-HT 显示出抗抑郁样作用。
Cas No.:78263-90-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects[1].
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) significantly decreases time of immobility thus showing anti-depressive-like effects[1]. Animal Model: Male Sprague-Dawley rats[1]
[1]. Sumaya IC, et al. Differential effects of a short-term high-fat diet in an animal model of depression in rats treated with the 5-HT3 receptor antagonist, ondansetron, the 5-HT3 receptor agonist, 2-methyl-5-HT, and the SSRI, fluoxetine. Pharmacol Biochem Behav. 2016 May;144:78-84.
| Cas No. | 78263-90-8 | SDF | |
| 别名 | 2-甲基-5-羟基色氨酸盐酸,2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT | ||
| Canonical SMILES | OC1=CC2=C(NC(C)=C2CCN)C=C1 | ||
| 分子式 | C11H14N2O | 分子量 | 190.24 |
| 溶解度 | DMSO: 125 mg/mL (657.06 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 5.2565 mL | 26.2826 mL | 52.5652 mL |
| 5 mM | 1.0513 mL | 5.2565 mL | 10.513 mL |
| 10 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Differential effects of a short-term high-fat diet in an animal model of depression in rats treated with the 5-HT3 receptor antagonist, ondansetron, the 5-HT3 receptor agonist, 2-Methyl-5-HT, and the SSRI, fluoxetine
Pharmacol Biochem Behav 2016 May;144:78-84.PMID:26979154DOI:10.1016/j.pbb.2016.03.005.
Investigation into the effects of a high-fat diet on depression in the context of 5-HT3 receptor function is important given 5-HT3 antagonism may represent a novel candidate for drug discovery. To more fully understand the relationship between the 5-HT3 receptor system, depression, and high-fat intake, our main interest was to study the short-term effects of a high-fat diet on the 5-HT3 receptor antagonist, ondansetron, and the 5-HT3 receptor agonist, 2-Methyl-5-HT, as well as the SSRI, fluoxetine, in an animal model of depression. Male Sprague Dawley rats were fed either a standard diet (11% fat) or a high-fat diet (32.5% fat) for seven days then treated with either fluoxetine (10mg/kg, ip), ondansetron (1mg/kg, ip), 2-Methyl-5-HT (3mg/kg, ip), fluoxetine+ondansetron or, 2-Methyl-5-HT+ondansetron prior to the Forced Swim Test. In the standard diet group, treatment with the 5HT3 receptor agonist, 2-Methyl-5-HT, served to significantly decrease time of immobility as compared to controls thus showing anti-depressive-like effects. Treatment with the 5-HT3 receptor antagonist, ondansetron, served to enhance the anti-depressive like effects of the SSRI, fluoxetine, as treatment with both the SSRI and 5-HT3 receptor antagonist dramatically decreased immobility. Importantly, in the high-fat diet groups, a week of high-fat intake served to: 1) counteract the anti-depressive-like effect of the SSRI, fluoxetine, 2) reverse the anti-depressive-like effect of the 5HT3 receptor agonist, 2-Methyl-5-HT and 3) provide protection against the depressive-like effects induced by the Forced Swim Test as rats fed a high-fat diet displayed the lowest amounts of immobility. In the aggregate, these data suggest that both SSRIs and the 5HT3 receptor system are affected by short-term high-fat intake and that a short-term high-fat diet protects against depressive-like effects in an animal model of depression.
Pre- and post-synaptic effects of the 5-HT3 agonist 2-Methyl-5-HT on the 5-HT system in the rat brain
Synapse 1995 May;20(1):54-67.PMID:7624830DOI:10.1002/syn.890200109.
Microiontophoretic applications of 5-HT and of the 5-HT3 agonist 2-Methyl-5-HT produced a current-dependent suppression of firing activity of both hippocampal (CA1 and CA3) and cortical neurons in anesthetized rats. Concomitant microiontophoretic applications of the 5-HT3 antagonists BRL 46470A and S-zacopride, as well as their intravenous injection, did not antagonize the inhibitory effect of 5-HT and 2-Methyl-5-HT. In contrast, the 5-HT1A antagonist BMY 7378, applied by microiontophoresis or administered intravenously, significantly reduced the inhibitory action of 5-HT and 2-Methyl-5-HT. The firing activity of dorsal raphe 5-HT neurons was also reduced by 5-HT, 2-Methyl-5-HT and the 5-HT1A agonist 8-OH-DPAT applied by microiontophoresis. While BRL 46470A (0.1 and 1 mg/kg, i.v.) did not antagonize the inhibitory effect of the three 5-HT agonists on 5-HT neuronal firing activity, only that of 8-OH-DPAT was attenuated by the 5-HT1A antagonist (+) WAY 100135. R-zacopride significantly reduced the duration of suppression of firing activity of CA3 pyramidal neurons induced by the electrical stimulation of the ascending 5-HT pathway, and this reducing effect was prevented by the three 5-HT3/5-HT4 antagonists renzapride, S-zacopride and tropisetron, but not by BRL 46470A. Finally, in in vitro superfusion experiments, both BRL 46470A and S-zacopride antagonized the enhancing action of 2-Methyl-5-HT on the electrically-evoked release of [3H]-5-HT in both rat frontal cortex and hippocampus slices. These findings suggest that, in vivo, the suppressant effect of 2-Methyl-5-HT on the firing activity of dorsal hippocampus pyramidal, somatosensory cortical, and dorsal raphe 5-HT neurons is not mediated by 5-HT3 receptors, but rather by 5-HT1A receptors. The attenuating effect of R-zacopride on the effectiveness of the stimulation of the ascending 5-HT pathway is not mediated by 5-HT3 receptors. In contrast, in vitro, the enhancing action of 2-Methyl-5-HT on the electrically-evoked release of [3H]5-HT in both frontal cortex and hippocampus slices is mediated by 5-HT3 receptors.
Ventral tegmental area 5-HT receptors: mesolimbic dopamine release and behavioural studies
Behav Brain Res 1996;73(1-2):1-5.PMID:8788468DOI:10.1016/0166-4328(96)00061-7.
Serotoninergic neurones originating in the dorsal and median raphe nuclei project to mesolimbic structures, including the nucleus accumbens (NAcb) and the ventral tegmental area (VTA), where they may have an important regulatory role. Some evidence from dopamine release, behavioural and binding studies directly implicates involvement of 5-HT3 and 5-HT4 receptors in the NAcb. Other in vivo dopamine release and behavioural experiments in rats have provided evidence for 5-HT3 receptor-mediated enhancement of mesolimbic dopaminergic activity, although the location of the 5-HT3 receptors involved is unknown because the selective 5-HT3 receptor agents used were administered systemically or intracerebroventricularly. This raises the possibility of a VTA site of action; as yet, however, relatively little is specifically known about 5-HT receptors and function in the VTA. Mesolimbic dopamine release in rats, measured in-vivo with microdialysis probes in the NAcb, can be inhibited by tropisetron administered directly into the VTA. In our laboratory, behavioural studies in rats have shown that a sustained hyperlocomotion is produced by 2-Methyl-5-HT administered into the VTA via stereotactically implanted guide cannulae. Mesolimbic dopaminergic activation is involved, because pretreatment with the catecholamine synthesis inhibitor alpha-methyl-p-tyrosine abolishes 2-methyl-5-HT-induced hyperlocomotion. The 2-Methyl-5-HT hyperlocomotor response is blocked by prior intra-VTA injection of ondansetron but is not affected by methiothepin, and intra-VTA 5-carboxamidotryptamine, alpha-methyl-5-HT or renzapride were without effect, thus a 5-HT3 receptor in the VTA mediates the 2-Methyl-5-HT response. These in vivo dopamine release and behavioural studies therefore confirm that 5-HT3 receptors in the VTA can mediate increased locomotor activity, by modulating the firing of mesolimbic dopaminergic cell bodies.
5-HT receptor subtypes outside the central nervous system. Roles in the physiology of the gut
Neuropsychopharmacology 1990 Oct-Dec;3(5-6):385-95.PMID:2078274doi
5-Hydroxytryptamine (5-HT) receptors have been analyzed and related to potential roles played by 5-HT in the physiology of the enteric nervous system (ENS). Three subtypes of 5-HT receptor--5-HT1P, 5-HT3, and 5-HT1A--have been found on enteric neurons. Receptors have been identified by intracellularly recording the electrical activity of enteric neurons and by studying the binding of radioligands and polyclonal anti-idiotypic antibodies raised against antibodies to 5-HT. Radioligand binding has been assessed by rapid filtration and by radioautography. 5-HT1P receptors mediate slow depolarizations of myenteric neurons that are associated with a closure of K+ channels. These responses can be inhibited by N-acetyl-hydroxytryptophyl-5-hydroxytryptophan amide (5-HTP-DP) and by the substituted benzamide, BRL 24924. 5-HT1P-like responses can be mimicked by 5- and 6-hydroxyindalpine, by another substituted benzamide, the S stereoisomer of zacopride, and by anti-idiotypic antibodies. 5-HT1P receptors can be labeled by 3H-5-HT and 3H-5-hydroxyindalpine with high affinity and are located on neurons of both enteric plexuses and on processes of intrinsic neurons in the gastrointestinal mucosa. A similar distribution of binding sites for anti-idiotypic antibodies is revealed by immunocytochemistry. Excitatory postsynaptic potentials (EPSPs) mediated by 5-HT are abolished by 5-HT1P antagonists. Blockade of 5-HT1P receptors is accompanied by acceleration of the rate of gastric emptying. Mucosal application of cholera toxin activates enteric neurons in both plexuses; this action is blocked by 5-HT1P or 5-HT3 antagonists and by anti-idiotypic antibodies. 5-HT3 receptors are responsible for fast depolarizations associated with increased membrane conductance. These responses are antagonized by ICS 205-930 and mimicked by 2-Methyl-5-HT and anti-idiotypic antibodies. 5-HT1A receptors have been reported to mediate hyperpolarizing responses associated with a rise in membrane conductance. Hyperpolarizing responses are also elicited by the 5-HT1A agonists, 8-hydroxy-di-n-propylaminotetralin (8-OH-DPAT) and 5-carboxyamidotryptamine. It is proposed that 5-HT1P receptors and perhaps 5-HT3 receptors are involved in initiating the peristaltic reflex and in regulating gastric emptying. No physiologic role has yet been identified for 5-HT1A receptors in the ENS.
Rabbit isolated renal artery contractions by some tryptamine derivatives, including 2-Methyl-5-HT, are mediated by a 5-HT1-like receptor
Br J Pharmacol 1992 Oct;107(2):322-8.PMID:1422584DOI:10.1111/j.1476-5381.1992.tb12745.x.
1. Despite the fact that 5-hydroxytryptamine (5-HT)-induced contractions of the rabbit isolated renal artery are mediated by a receptor belonging to the heterogeneous 5-HT1-like category, we observed that the so-called selective 5-HT3 receptor agonist, 2-Methyl-5-HT, caused a concentration-dependent contraction of this vessel. This study was therefore undertaken to analyze the effects of 2-Methyl-5-HT in the renal artery segments, either quiescent or precontracted with U46619 (10(-7) M). alpha-Methyl-5-HT and 5-methoxytryptamine, which have high affinities for 5-HT2 and 5-HT4 receptors, respectively, were used for comparison. 2. In the precontracted vessel segments, the maximum contractile responses obtained with 2-Methyl-5-HT, alpha-methyl-5-HT, 5-methoxytryptamine and 5-HT were similar to those in the quiescent segments. However the pD2 values were higher in the precontracted segments, making them about 4-100 fold more sensitive. 3. Neither MDL 72222 (10(-6) M) nor tropisetron (3 x 10(-6) M) suppressed renal artery contractions elicited by 5-HT, 2-Methyl-5-HT, alpha-methyl-5-HT or 5-methoxytryptamine, thus ruling out the involvement of 5-HT3 as well as 5-HT4 receptors. 4. On the other hand, both methiothepin (10(-8) and 10(-7) M) and ketanserin (10(-7) and 10(-6) M) caused a rightward shift of agonist concentration-effect curves.The two antagonists had similar pA2 values against the different agonists tested on either quiescent or precontracted vessels, but ketanserin (apparent pA2: 6.6 to 7.0) was between 20-100 fold less potent than methiothepin (apparent pA2: 8.4 to 8.8).5. The results of this functional study permit us to conclude that the contractile effects of 2-Methyl-5-HT as well as ct-methyl-5-HT and 5-methoxytryptamine on the rabbit isolated renal artery are mediated by a 5-HT1-like receptor. Since, in addition, the reported ligand binding affinity of 2-Methyl-5-HT at 5-HT3 receptors is similar to both the ligand binding affinity and the functional pD2 at 5-HTI sites, this compound cannot be regarded as a selective 5-HT3 receptor agonist. Similarly, a-methyl-5-HT and 5-methoxytryptamine have only a limited selectivity for 5-HT2 and 5-HT4 receptors, respectively.