RTI-31
(Synonyms: RTI-COC 31) 目录号 : GC45607
An Analytical Reference Standard
Cas No.:130342-80-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
RTI-31 is an analytical reference standard that is categorized as a tropane. RTI-31 increases self-administration in rhesus monkeys.1 This product is intended for research and forensic applications.
|1. Wee, S., Carroll, F.I., and Woolverton, W.L. A reduced rate of in vivo dopamine transporter binding is associated with lower relative reinforcing efficacy of stimulants. Neuropsychopharmacology 31(2), 351-362 (2006).
| Cas No. | 130342-80-2 | SDF | |
| 别名 | RTI-COC 31 | ||
| Canonical SMILES | ClC(C=C1)=CC=C1[C@H]2C[C@@H]3CC[C@@H](N3C)[C@H]2C(OC)=O | ||
| 分子式 | C16H20ClNO2 | 分子量 | 293.8 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 30 mg/ml | 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 | 3.4037 mL | 17.0184 mL | 34.0368 mL |
| 5 mM | 0.6807 mL | 3.4037 mL | 6.8074 mL |
| 10 mM | 0.3404 mL | 1.7018 mL | 3.4037 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。
Interaction of tyrosine 151 in norepinephrine transporter with the 2β group of cocaine analog RTI-113
Neuropharmacology 2011 Jul-Aug;61(1-2):112-20.PMID:21420984DOI:10.1016/j.neuropharm.2011.03.014.
Cocaine binds and inhibits dopamine transporter (DAT), norepinephrine transporter (NET) and serotonin transporter. The residues forming cocaine binding sites are unknown. RTI-113, a cocaine analog, is 100× more potent at inhibiting DAT than inhibiting NET. Here we show that removing the hydroxyl group from residue Tyr151 in NET by replacing it with Phe, the corresponding residue in DAT, increased the sensitivity of NET to RTI-113, while the reverse mutation in DAT decreased the sensitivity of DAT to RTI-113. In contrast, RTI-31, another cocaine analog having the same structure as RTI-113 but with the phenyl group at the 2β position replaced by a methyl group, inhibits the transporter mutants equally well whether a hydroxyl group is present at the residue or not. The data suggest that this residue contributes to cocaine binding site and is close to the 2β position of cocaine analogs. These results are consistent with our previously proposed cocaine-DAT binding model where cocaine initially binds to a site that does not overlap with, but is close to, the dopamine-binding site. Computational modeling and molecular docking yielded a binding model that explains the observed changes in RTI-113 inhibition potencies.
Rate of binding of various inhibitors at the dopamine transporter in vivo
Psychopharmacology (Berl) 1995 Jun;119(4):376-84.PMID:7480516DOI:10.1007/BF02245852.
The rate of entry of drugs into brain is thought to be a factor in their abuse liability. In this investigation, we have examined the rate of entry and binding at dopamine transporters in mouse striatum for a variety of dopamine transporter inhibitors. The method utilized was based on measuring the displacement of 3H-WIN 35,428 from striatal dopamine transporter sites in vivo at different times. Eleven cocaine analogs (RTI-31, RTI-32, RTI-51, RTI-55, RTI-113, RTI-114, RTI-117, RTI-120, RTI-121, WIN 35,065-2, and WIN 35,428) as well as other dopamine uptake site blockers (bupropion, nomifensine, and methylphenidate) were compared with (-) cocaine for their rates of displacement of 3H-WIN 35,428 binding in vivo. The drugs that displayed the fastest occupancy rates were bupropion, (-) cocaine, nomifensine, and methylphenidate. RTI-51, RTI-121, RTI-114, RTI-117, RTI-120, RTI-32, RTI-55, and RTI-113, showed intermediate rates, whereas RTI-31, WIN 35,065-2, and WIN 35,428 exhibited the slowest rates of displacement. While many of the cocaine analogs have proven to be behaviorally and pharmacologically more potent than (-) cocaine, their rates of entry and binding site occupancy were slower than that for (-) cocaine. Earliest times of transporter occupancy by the different drugs were correlated (although weakly) with their degree of lipophilicity (r = 0.59; P < 0.02). Kinetic effects and metabolism of the compounds could complicate the interpretations of these data.(ABSTRACT TRUNCATED AT 250 WORDS)
Locomotor stimulant effects of cocaine and novel cocaine analogs in DBA/2J and C57BL/6J inbred mice
Pharmacol Biochem Behav 1995 Feb;50(2):163-9.PMID:7740054DOI:10.1016/0091-3057(94)00277-p.
The current study compared the potencies of cocaine and a series of substituted phenyltropane analogs of cocaine in stimulating locomotor activity in two genetically distinct strains of mice previously shown to differ in their locomotor responsiveness to cocaine. In addition, these compounds were compared for their abilities to induce stereotyped behaviors in naive and cocaine-pretreated mice. All of the analogs tested were more potent locomotor stimulants than cocaine in both strains. Interstrain differences in the locomotor stimulant efficacy of RTI-31 and RTI-98 parallel those of cocaine, with DBA/2J mice being stimulated to a greater extent than C57BL/6J mice at maximally active doses. Significant differences exist in the onset and duration of action among cocaine and several analogs. Whereas the action of cocaine peaks in the first 10 min after injection and thereafter rapidly declines, the stimulant effects of RTI-31, RTI-98, and RTI-113 are maximal at 30-40 min and remain consistent through 60 min postinjection. The current results are discussed in the context of previously published reports of genotype-dependent differences in behavioral responsiveness to cocaine in the DBA/2J and C57BL/6J strains.
Relationships among dopamine transporter affinities and cocaine-like discriminative-stimulus effects
Psychopharmacology (Berl) 2000 Jan;148(1):90-8.PMID:10663422DOI:10.1007/s002130050029.
Rationale: The discriminative-stimulus effects of cocaine have been reported to be mediated by indirect agonist actions initiated by the blockade of dopamine uptake, and the potencies of drugs that have discriminative-stimulus effects like cocaine are directly related to their dopamine transporter binding affinities. The binding to the dopamine transporter by cocaine and many of its analogs has been reported to fit better using a two-site model than a one-site model. Objectives: The present study examined the relationship among binding affinities of dopamine uptake inhibitors at these two sites and their potencies to produce discriminative-stimulus effects. Methods: The inhibition constants (K(i) values) were derived for unlabeled dopamine uptake inhibitors for displacement of [(3)H]WIN 35,428 from rat caudate putamen membranes. These K(i) values were related to the ED(50) values obtained in rats trained to discriminate 10 mg/kg cocaine from saline injections under a fixed-ratio 20 schedule of food reinforcement. Results: Among the dopamine uptake inhibitors studied, the binding data for eight compounds (WIN 35,428, nomifensine, WIN 35,981, WIN 35,065-2, methylphenidate, cocaine, cocaethylene, and bupropion) were better fit by a two-site model than a one-site model. The data for the remaining eleven compounds (RTI-31, RTI-55, RTI-121, RTI-32, LU19-005, BTCP, GBR12909, GBR12935, mazindol, LU17-133, and EXP561) were better fit by a one-site model. Of the drugs that were fit best by a two-site model, there was a higher correlation among the K(i) values for the high-affinity site and the ED(50) values (R(2)=0.655; P=0.015) than there was for the low-affinity site (R(2)=0.543; P=0. 037). Of the remaining drugs, there was a high correlation among the K(i) values and the ED(50) values for the discriminative-stimulus effects (R(2)=0.523; P=0.012). Conclusions: These data suggest that the discriminative-stimulus effects of cocaine are more closely related to actions mediated by high-affinity binding to the dopamine transporter than they are to actions mediated by the low-affinity site. The further assessment of the respective contributions of high- and low-affinity binding to the behavioral effects of cocaine will be greatly enhanced with the development of pharmacological tools that have a high degree of selectivity for one of these components.
Rate of onset of dopamine transporter inhibitors assessed with intracranial self-stimulation and in vivo dopamine photometry in rats
Psychopharmacology (Berl) 2023 Apr;240(4):969-981.PMID:36802016DOI:10.1007/s00213-023-06340-8.
Drug self-administration and intracranial self-stimulation (ICSS) are two preclinical behavioral procedures used to predict abuse potential of drugs, and abuse-related drug effects in both procedures are thought to depend on increased mesolimbic dopamine (DA) signaling. Drug self-administration and ICSS yield concordant metrics of abuse potential across a diverse range of drug mechanisms of action. The "rate of onset," defined as the velocity with which a drug produces its effect once administered, has also been implicated as a determinant of abuse-related drug effects in self-administration procedures, but this variable has not been systematically examined in ICSS. Accordingly, this study compared ICSS effects produced in rats by three DA transporter inhibitors that have different rates of onset (fastest to slowest: cocaine, WIN-35428, RTI-31) and that produced progressively weaker metrics of abuse potential in a drug self-administration procedure in rhesus monkeys. Additionally, in vivo photometry using the fluorescent DA sensor dLight1.1 targeted to the nucleus accumbens (NAc) was used to assess the time course of extracellular DA levels as a neurochemical correlate of behavioral effects. All three compounds produced ICSS facilitation and increased DA levels assessed by dLight. In both procedures, the rank order of onset rate was cocaine > WIN-35428 > RTI-31; however, in contrast to monkey drug self-administration results, maximum effects did not differ across compounds. These results provide additional evidence that drug-induced increases in DA drive ICSS facilitation in rats and illustrate the utility of both ICSS and photometry to evaluate the time course and magnitude of abuse-related drug effects in rats.