GR 127935 hydrochloride是一种5-HT1B/1D受体拮抗剂，可抑制降压反应。
Cas No.:148642-42-6
Sample solution is provided at 25 µL, 10mM.
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GR 127935 hydrochloride is a 5-HT1B/1D receptor antagonist that inhibits hypotensive responses [1]. GR 127935 hydrochloride can irreversibly antagonize the contraction of isolated canine basilar arteries and veins induced by sumatriptan, persistently antagonize hypothermia and rotational behavior mediated by 5-HT 1D receptors in guinea pigs, and block the central 5-HT1D auto-receptors both in vitro and in vivo[2]. GR 127935 hydrochloride has been widely used to regulate the basic locomotor activity of rats and prevent excessive activity [3].
In vitro, GR 127935 hydrochloride treatment for 48 hours significantly inhibited the replication of SARS-CoV-2 virus in HEK293T-ACE2-TMPRSS2 cells, with an EC50 value of 1.6µM[4].
In vivo, GR 127935 hydrochloride treatment via a single subcutaneous injection at a dose of 3mg/kg for 1 hour significantly reversed the increase in the brain reward threshold caused by RU 24969 (1mg/kg) in rats[5]. A single intraperitoneal injection of GR 127935 hydrochloride (10mg/kg) significantly reduced the 1-hour movement distance and decreased the axillary temperature in adult male and female rats[6].
References:
[1] Sánchez-Maldonado C, López-Sánchez P, Anguiano-Robledo L, et al. GR-127935-sensitive Mechanism Mediating Hypotension in Anesthetized Rats: Are 5-HT: 5B: Receptors Involved?[J]. Journal of Cardiovascular Pharmacology, 2015, 65(4): 335-341.
[2] Skingle M, Beattie D T, Scopes D I C, et al. GR127935: a potent and selective 5-HT1D receptor antagonist[J]. Behavioural brain research, 1995, 73(1-2): 157-161.
[3] Chaouloff F, Courvoisier H, Moisan M P, et al. GR 127935 reduces basal locomotor activity and prevents RU 24969-, but not D-amphetamine-induced hyperlocomotion, in the Wistar-Kyoto hyperactive (WKHA) rat[J]. Psychopharmacology, 1999, 141(3): 326-331.
[4] Nehul S, Nagaraj S K, Narayan R, et al. A novel molecule inhibits SARS-CoV-2 RBD binding to the ACE2 receptor, blocks viral entry and exhibits antiviral activity in a murine model[J]. Archives of Virology, 2026, 171(3): 98.
[5] Harrison A A, Parsons L H, Koob G F, et al. RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist[J]. Psychopharmacology, 1999, 141(3): 242-250.
[6] McDougall S A, Roe M J, Robinson J A M, et al. Effects of the serotonin 5-HT1B receptor agonist CP 94253 on the locomotor activity and body temperature of preweanling and adult male and female rats[J]. European Journal of Pharmacology, 2022, 926: 175019.
GR 127935 hydrochloride是一种5-HT1B/1D受体拮抗剂，可抑制降压反应[1]。GR 127935 hydrochloride能不可逆地拮抗sumatriptan诱导的离体犬基底动脉和静脉收缩，持久拮抗豚鼠中由5-HT1D受体介导的体温降低和旋转行为，并在体外和体内阻断中枢5-HT1D自身受体[2]。GR 127935 hydrochloride已被广泛用于调节大鼠的基础运动活性并防止过度活动[3]。
在体外，GR 127935 hydrochloride处理 HEK293T-ACE2-TMPRSS2细胞48小时，显著抑制了SARS-CoV-2病毒的复制，EC50值为1.6µM[4]。
在体内，单次皮下注射3mg/kg剂量的GR 127935 hydrochloride 1小时，显著逆转了RU 24969 (1mg/kg)引起的大鼠脑内奖赏阈值的升高[5]。单次腹腔注射10mg/kg剂量的GR 127935 hydrochloride，显著减少了成年雄性和雌性大鼠在1小时内的移动距离，并降低了腋下温度[6]。
| Cell experiment [1]: | |
Cell lines | HEK293T-ACE2-TMPRSS2 cells |
Preparation Method | HEK293T-ACE2-TMPRSS2 cells were maintained in high glucose DMEM complemented with 10% FBS, 100units of penicillin, and 100µg/ml streptomycin in a humidified incubator at 37°C and 5% CO2. The day before the pseudovirus assay, HEK-293T-hACE2-TMPRSS2 cells (0.5×106 cells per well) were seeded into a gelatin-coated 96-well plate (0.1%). The next day, two-fold serial dilutions of GR 127935 hydrochloride were prepared in 2% DMEM, producing final concentrations (0.02, 0.1, 1, 5, 10, and 15μM). The serially diluted GR 127935 hydrochloride was mixed in equal volumes with the virus (1×106 RLU/mL) supplemented with 10mg/ml hexadimethrine bromide and incubated for 30min at 37°C in a 5% CO2 incubator. Subsequently, each dilution was then added to HEK-293T cells expressing human ACE2-TMPRSS2. The plate was then incubated at 37°C in a 5% CO2 incubator for 60h, after which the cell lysate was prepared and used for the luciferase assay. |
Reaction Conditions | 0.02, 0.1, 1, 5, 10, and 15μM; 60h |
Applications | GR 127935 hydrochloride treatment significantly inhibited the entry of pseudovirus particles into HEK293T-ACE2-TMPRSS2 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats |
Preparation Method | Sprague-Dawley rats were housed in large polycarbonate maternity cages on ventilated racks at 22-23°C and kept under a 12:12 light/dark cycle. Food and water were freely available. Behavioral testing was done in activity monitoring chambers that consisted of acrylic walls, a plastic floor, and an open top. Each chamber included an X-Y photobeam array, with 16 photocells and detectors, that was used to determine distance traveled (locomotor activity). Rats were injected intraperitoneally with saline vehicle or GR 127935 hydrochloride (10mg/kg) and immediately placed in activity chambers, where distance traveled (i.e., horizontal locomotor activity) was measured for 60min. |
Dosage form | 10mg/kg for once; i.p. |
Applications | GR 127935 hydrochloride treatment significantly reduced the 1-hour movement distance in rats. |
References: | |
| Cas No. | 148642-42-6 | SDF | |
| 化学名 | N-(4-methoxy-3-(4-methylpiperazin-1-yl)phenyl)-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-carboxamide hydrochloride | ||
| Canonical SMILES | O=C(C(C=C1)=CC=C1C2=CC=C(C3=NOC(C)=N3)C=C2C)NC4=CC=C(C(N5CCN(C)CC5)=C4)OC.Cl | ||
| 分子式 | C29H31N5O3.HCl | 分子量 | 534.06 |
| 溶解度 | DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.25 mg/ml | 储存条件 | Store at 2-8°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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8724 mL | 9.3622 mL | 18.7245 mL |
| 5 mM | 374.5 μL | 1.8724 mL | 3.7449 mL |
| 10 mM | 187.2 μL | 936.2 μL | 1.8724 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，
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2.
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