2. U-11634

U-11634 是一种口服有效的多巴胺 β-羟化酶 (dopamine β-hydroxylase) 非竞争性抑制剂，对大鼠的 LD50 值为 1197 mg/kg (皮下注射) 和 524 mg/kg (口服)。U-11634 可阻断多巴胺 (dopamine) 向去甲肾上腺素 (norepinephrine) 的转化，并可降低脑内的去甲肾上腺素水平。U-11634 通过膳食添加的方式降低食物摄入量与自主运动活性。U-11634 可诱发甲状腺毒性，抑制妊娠。U-11634可用于妊娠的研究。

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U-11634

U-11634 Chemical Structure

CAS No. : 3414-47-9

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U-11634 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

U-11634 is an orally active dopamine β-hydroxylase noncompetitive inhibitor, with rat LD50 values of 1197 mg/kg (subcutaneous) and 524 mg/kg (oral). U-11634 blocks conversion of dopamine to norepinephrine and reduces norepinephrine levels in brain. U-11634 decreases food intake and spontaneous motor activity via dietary inclusion. U-11634 induces thyroid toxicity and inhibits pregnancy. U-11634 inhibits deciduomata formation in intact and steroid-treated rats, with no reversal by progesterone or oestradiol. U-11634 can be used for pregnancy[1][2][3][4].

体外研究
(In Vitro)

U-11634 (compound 12) (1×10-4 M) 可在体外中度抑制纯化的牛肾上腺多巴胺 β-羟化酶，通过非竞争性抑制将酶活性降至对照组的 52%[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

U-11634 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Serum Concentration
Rat[3] 100 mg/kg p.o. 10.0 μg/mL
Cynomolgus Monkey[3] 200 mg/kg p.o. 10.4 μg/mL
体内研究
(In Vivo)

U-11634 (compound 12) (200 mg/kg；腹腔注射；单剂量) 在单次 200 mg/kg 腹腔注射后 4 小时可将大鼠脑内去甲肾上腺素水平降至对照组的 82%，16 小时时降至对照组的 72%[1]。
U-11634 (每 24 小时 616 mg/kg；口服；单次给药；持续 24 小时) 可将小鼠的自主活动能力降至对照组的 67%[1]。
U-11634 (5-10 mg/天；每日皮下注射；连续 20 天) 不会改变处于发情周期的成年 Sprague-Dawley 雌性大鼠的阴道细胞学特征、体重增长、治疗后交配间隔或产仔结局[2]。
U-11634 (每日 5-10 mg；皮下注射；每日 1 次；假妊娠第 4、5、6 天) 对 Sprague-Dawley 大鼠从假妊娠开始至首次给药后动情样涂片的间隔时间无显著改变[2]。
U-11634 (25 mg；口服；单剂量) 经口服给予雌性 Sprague-Dawley 大鼠后，会被快速吸收，在 2 小时时达到 13.3 μg/mL 的血清峰值 (按 100 mg/kg 标准化)，且血清药物浓度可稳定维持长达 24 小时[3]。
U-11634 (200 mg/kg；口服；单次给药) 经口服给予雄性 cynomologous 猴后，表现出吸收缓慢的特征，两只动物在 12 小时时的血清峰值分别为 33.0 μg/mL 和 49.4 μg/mL，且在 24 小时内代谢/排泄缓慢[3]。
U-11634 (0.25-10 mg；皮下注射；从发情前期至第 6 天每日给药；在第 2、4、6、12 或 16 天单次给药；从第 1 天至第 3 天每日给药；从第 3 天至第 6 天每日给药) 可在着床前早期阶段完全抑制 Sprague-Dawley 大鼠的妊娠，且治疗剂量下未观察到胚胎毒性[4]。
U-11634 (3-12 mg/rat；膳食给药；从发情前期至第 6 天的平均每日摄入量) 可在着床前早期阶段完全抑制 Sprague-Dawley 大鼠的妊娠，且治疗剂量下未观察到胚胎毒性[4]。
U-11634 (1.0-5.0 mg/rat；口服；从发情前期开始每日给药 7 天或 13 天) 可在着床前早期阶段完全抑制 Sprague-Dawley 大鼠的妊娠，且治疗剂量下未观察到胚胎毒性[4]。
U-11634 (1.0-5.0 mg；皮下注射；第 1 天至第 8 天每日给药) 可抑制小鼠的妊娠[4]。
U-11634 (0.25 mg/只小鼠；口服；第 1 天至第 8 天每日给药) 可显著抑制小鼠的妊娠[4]。
U-11634 (每只大鼠 0.05-6.4 mg；皮下注射；每日 1 次，连续 10 天) 在抗生育剂量下对未成年雄性 Sprague-Dawley 大鼠无促性腺激素抑制活性，仅在治疗剂量 4 倍时观察到对生殖组织的轻微作用[4]。
U-11634 (0.05-2.0 mg；口服；每日给药，连续 10 天) 在每日口服剂量高达 2.0 mg/rat 时，未在双侧卵巢切除的未成年 Sprague-Dawley 大鼠中表现出子宫增重活性或抗雌激素活性[4]。
U-11634 (每只大鼠 0.5-8.0 mg；口服；连续给药 10 天) 在去势雄性幼年 Sprague-Dawley 大鼠中，即使每日口服剂量高达 8.0 mg/rat，也未表现出雄激素活性[4]。
U-11634 (10 mg/只大鼠；口服；第 5 天至第 8 天每日给药) 可抑制完整以及经激素处理的去卵巢假孕 Sprague-Dawley 大鼠的蜕膜形成，支持干扰子宫内膜蜕膜化是其抑制妊娠的作用机制[4]。
U-11634 (12.5-50 mg/kg；口服；妊娠第 9 天至第 15 天每日给药) 在妊娠中期每日口服剂量高达 50 mg/kg 时，不会对妊娠 Sprague-Dawley 大鼠造成显著的胎仔毒性、死亡或发育异常[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (male, 140-200 g)[1]
Dosage: 200 mg/kg
Administration: i.p.; single dose
Result: Remained at 100% of control values at 2 hours post-dose.
Reduced to 82% of control values at 4 hours post-dose.
Reduced to 72% of control values at 16 hours post-dose.
Animal Model: CF-1 (male)[1]
Dosage: 616 mg/kg
Administration: p.o.; single application for 24 h
Result: Reduced spontaneous motor activity to 67% of control values.
Animal Model: Sprague-Dawley (mature female, cyclic)[2]
Dosage: 5 mg/day; 10 mg/day
Administration: s.c.; daily; 20 days
Result: Showed no effect on vaginal cytology relative to vehicle controls.
Did not significantly differ from controls in body-weight gain (5 mg/day group: +25 g; 10 mg/day group: +23 g), days from end of treatment to mating (5 mg/day group: 2.0 days; 10 mg/day group: 3.6 days), litter size (5 mg/day group: 11.6 foetuses; 10 mg/day group: 11.2 foetuses), average foetal weight (5 mg/day group: 2.9 g; 10 mg/day group: 2.6 g), and foetal gross condition.
Animal Model: Sprague-Dawley (lactating, litters reduced to 8 pups)[2]
Dosage: 10 mg/day
Administration: s.c.; once daily; days 5, 6, 7 of lactation
Result: Showed no effect on pup weight (pups gained an average of 1.5 g body weight daily) or pup survival (no pup deaths) relative to controls.
Showed no effect on vaginal cytology timing (cornified oestrous smears observed on day 18 or 19, matching control timing) relative to controls.
Animal Model: Sprague-Dawley (female, 219-231 g)[3]
Dosage: 100 mg/kg
Administration: p.o.; single dose
Result: Reached normalized serum level of 10.0 μg/mL at 1 hour.
Reached normalized serum level of 13.3 μg/mL at 2 hours.
Reached normalized serum level of 14.2 μg/mL at 4 hours.
Reached normalized serum level of 12.8 μg/mL at 6 hours.
Reached normalized serum level of 14.4 μg/mL at 8 hours.
Reached normalized serum level of 15.8 μg/mL at 12 hours.
Reached normalized serum level of 10.0 μg/mL at 18 hours.
Reached normalized serum level of 15.3 μg/mL at 24 hours.
Observed peak levels 1-2 hours post-administration.
Maintained relatively stable serum levels from 2-24 hours.
Animal Model: Two Macaca irus (male, weighing 4 kg and 5 kg, respectively)[3]
Dosage: 200 mg/kg
Administration: p.o.; single dose
Result: Reached serum level of 10.4 μg/mL at 2 hours in monkey No. 635.
Reached serum level of 20.0 μg/mL at 4 hours in monkey No. 635.
Reached serum level of 29.2 μg/mL at 6 hours in monkey No. 635.
Reached serum level of 32.6 μg/mL at 8 hours in monkey No. 635.
Reached serum level of 33.0 μg/mL at 12 hours in monkey No. 635.
Reached serum level of 14.7 μg/mL at 24 hours in monkey No. 635.
Reached serum level of 12.7 μg/mL at 2 hours in monkey No. 636.
Reached serum level of 24.6 μg/mL at 4 hours in monkey No. 636.
Reached serum level of 32.7 μg/mL at 6 hours in monkey No. 636.
Reached serum level of 42.4 μg/mL at 8 hours in monkey No. 636.
Reached serum level of 49.4 μg/mL at 12 hours in monkey No. 636.
Reached serum level of 50.4 μg/mL at 24 hours in monkey No. 636.
Observed peak levels at 12 hours or later post-administration.
Animal Model: Sprague-Dawley (mature nulliparous, 200 to 250 g body weight, pregnancy model via mating with fertile males)[4]
Dosage: 0.25 mg/rat; 1 mg/rat; 2.5 mg/rat; 5 mg/rat; 10 mg/rat
Administration: s.c.; daily from pro-oestrus to Day 6
Result: Completely inhibited pregnancy (0 decidual sites per rat) at subcutaneous doses of 2.5, 5.0, and 10 mg/rat daily from pro-oestrus to Day 6.
Animal Model: Mice (25-28 g body weight, pregnancy model)[4]
Dosage: 1.0 mg/mouse; 2.5 mg/,ouse; 5.0 mg/mouse
Administration: s.c.; daily from Day 1 to Day 8
Result: Inhibited pregnancy at subcutaneous doses of 1.0, 2.5, and 5.0 mg/mouse daily from Day 1 to Day 8, with only 1/5 mice showing reduced, non-progressing decidual sites at the 1.0 and 5.0 mg/mouse doses.
Animal Model: Mice (25-28 g body weight, pregnancy model)
[4]
Dosage: 0.05 mg/mouse; 0.10 mg/mouse; 0.25 mg/mouse; 1 mg/mouse; 5.0 mg/mouse
Administration: p.o.; daily from Day 1 to Day 8
Result: Significantly inhibited pregnancy at the minimal effective oral dose of 0.25 mg/mouse daily; complete pregnancy inhibition was not achieved with any tested oral dose.
Animal Model: Sprague-Dawley (immature male, 26 to 28 days of age)[4]
Dosage: 0.05 mg/rat; 0.8 mg/rat; 1.6 mg/rat; 3.2 mg/rat; 6.4 mg/rat
Administration: s.c.; daily for 10 days
Result: Observed no significant changes in testes, seminal vesicle, or levator ani weights, or body weight gain at 1.6 mg/rat (equivalent to minimal 100% effective anti-fertility dose) compared to controls.
Observed slight reductions in testes (1.10 g vs. 1.34 g control), seminal vesicle (12 mg vs. 17 mg control), and levator ani (25 mg vs. 33 mg control) weights, plus reduced body weight gain (42 g vs. 50 g control) at 6.4 mg/rat (four times the anti-fertility dose).
Animal Model: Sprague-Dawley (immature bilaterally ovariectomized, ~70 g body weight)[4]
Dosage: 0.05 mg/rat; 0.20 mg/rat; 0.40 mg/rat; 1.0 mg/rat; 2.0 mg/rat
Administration: p.o.; daily for 10 days
Result: Did not increase uterine weight compared to vehicle controls (average uterine weight 25.2 mg, not significantly different from controls) at any tested oral dose.
Did not significantly reduce the uterine weight increase induced by concomitant oestradiol administration (122 mg in oestradiol-only group, no significant difference with U-11634 co-administration) at any tested dose.
Animal Model: Sprague-Dawley (immature castrated male, ~100 g body weight)[4]
Dosage: 0.5 mg/rat; 8.0 mg/rat
Administration: p.o.; daily for 10 days
Result: Did not significantly increase seminal vesicle (control 6.0 mg) or prostate (control 32.2 mg) weights compared to vehicle controls at any tested oral dose.
Animal Model: Sprague-Dawley (pregnant females)[4]
Dosage: 12.5 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.; daily from Day 9 to Day 15 of pregnancy
Result: No significant differences between treated and control groups in average number of foetuses per litter, average foetal weight, crown-rump distance, number of implantation sites, or number of resorption sites.
No foetal deaths, and only one isolated foetal abnormality (no tail) in the 50 mg/kg group.
分子量

277.26

Formula

C11H10F3NO2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

U-11634 相关分类

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Keywords:

U-116343414-47-9U11634U 11634cynomologous monkeysdopamine β-hydroxylaseSprague-Dawley ratsbovine adrenaldopamineSwiss-Webster micedeciduomata formationthyroid toxicitypregnancynorepinephrineInhibitorinhibitorinhibit

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