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浣嶇疆锛欬a href="/">棣栭〉> 浜у搧搴掽/a> > (S)-UFR2709 hydrochloride
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*楠岃瘉鐮侊細
(S)-UFR2709 hydrochloride
鏈骇鍝佷笉鍚戜釜浜洪攢鍞紝浠呯敤浣滅瀛︾爺绌讹紝涓嶇敤浜庝换浣曚汉浣撳疄楠屽強闈炵鐮旀€ц川鐨勫姩鐗╁疄楠屻€侟/div>
(S)-UFR2709 hydrochloride鍥剧墖
鍖呰涓庝环鏍硷細
鍖呰 浠锋牸(鍏?
10 mM * 1 mL in DMSO 鐢佃
5mg 鐢佃
10mg 鐢佃
25mg 鐢佃
50mg 鐢佃
100mg 鐢佃
200mg 鐢佃
500mg 鐢佃

浜у搧浠嬬粛
(S)-UFR2709 (hydrochloride) 鏄竴绉嶇珵浜夋€х殑 nAChR鎷姉鍓傦紝骞舵樉绀哄嚭杈冨己鐨勪翰鍜屽姏锛屽 伪 4尾 2nAChR 鐨勪翰鍜屽姏姣斿 伪 7nAChR 鐨勯珮銆?S)-UFR2709 (hydrochloride) 鍦ㄥ亸濂介厭绮剧殑鑰侀紶涓噺灏戠劍铏戯紝骞朵笖鍙互鍑忓皯鍏堕厭绮炬憚鍏ュ拰瀵归厭绮惧亸濂姐€?S)-UFR2709 (hydrochloride) 鏄姉鐒﹁檻璇曞墏锛屽彲鐢ㄤ簬鐮旂┒灏煎彜涓佹垚鐦俱€侟/div>
鐢熺墿娲绘€?/td>

(S)-UFR2709 (hydrochloride) is a competitivenAChRantagonist and displays higher affinity for 伪4尾2nAChRs than for 伪7nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction[1][2].
浣撳鐮旂┒
(In Vitro)

Brain nicotinic acetylcholine receptors (nAChRs) is a heterogeneous family of pentameric acetylcholine-gated cation channels, which is a molecular target for the treatment of alcohol abuse and dependence[1].
浣撳唴鐮旂┒
(In Vivo)

(S)-UFR2709 (hydrochloride) (50-100 渭g/ml; 3 min and then maintained for another 5 min in a holding tank before testing the swimming behaviour in the test tank for a period of 5 min) produces a decrease in the bottom dwelling for NTT test, and UFR2709 induces a significant and dose-dependent decrease in bottom dwelling time to 52.9 and 87.0 s, respectively at 50 and 100 渭g/ml[2].
(S)-UFR2709 (hydrochloride) (50-100 渭g/ml) decreases nicotine-evoked mRNA expression of 伪4 nACh receptor subunit, but UFR2709 has less effect on 伪4 nACh receptor subunit in the brain of adult zebrafish[2].
(S)-UFR2709 (hydrochloride) (intraperitoneal injection; 1-10 mg/kg; daily; 17 days) reduces ethanol consumption and ethanol preference and increased water consumption in a dose-dependent manner. The most effective dose of UFR2709 is 2.5 mg/kg, it induces a 56% reduction in alcohol consumption. (S)-UFR2709 (hydrochloride) does not affect the weight or locomotor activity of the rats[1].

Animal Model: High-alcohol-drinking UChB rats[1]
Dosage: 10 mg/kg, 5 mg/kg, 2.5 mg/kg, or 1 mg/kg
Administration: Intraperitoneal injection; 1-10 mg/kg; daily; 17 days
Result: Did not affect the weight or locomotor activity and reduced ethanol consumption and preference.
鍒嗗瓙閲廃/td>

255.74
鎬х姸

Solid
Formula

C13H18ClNO2
杩愯緭鏉′欢

Room temperature in continental US; may vary elsewhere.
鍌ㄥ瓨鏂瑰紡

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
婧惰В鎬ф暟鎹?/td>
In Vitro:

H2O : 100 mg/mL(391.02 mM;Need ultrasonic)

DMSO : 50 mg/mL(195.51 mM;Need ultrasonic)

閰嶅埗鍌ㄥ娑秉/div>
娴撳害婧跺墏浣撶Н璐ㄩ噺 1 mg 5 mg 10 mg
1 mM 3.9102 mL 19.5511 mL 39.1022 mL
5 mM 0.7820 mL 3.9102 mL 7.8204 mL
10 mM 0.3910 mL 1.9551 mL 3.9102 mL
*

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鍌ㄥ娑茬殑淇濆瓨鏂瑰紡鍜屾湡闄愶細-80鈩? 6 months; -20鈩? 1 month (stored under nitrogen)銆侟/span>-80鈩 鍌ㄥ瓨鏃讹紝璇峰湪 6 涓湀鍐呬娇鐢紝-20鈩 鍌ㄥ瓨鏃讹紝璇峰湪 1 涓湀鍐呬娇鐢ㄣ€侟/span>

In Vivo:

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  • 1.

    璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 PBS

    Solubility: 50 mg/mL (195.51 mM); Clear solution; Need ultrasonic

  • 2.

    璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 10% DMSO40%PEG3005%Tween-8045% saline

    Solubility: 鈮 2.5 mg/mL (9.78 mM); Clear solution

    姝ゆ柟妗堝彲鑾峰緱 鈮 2.5 mg/mL (9.78 mM锛岄ケ鍜屽害鏈煡) 鐨勬緞娓呮憾娑层€侟/p>

    浠 1 mL 宸ヤ綔娑蹭负渚嬶紝鍙 100 渭L 25.0 mg/mL 鐨勬緞娓 DMSO 鍌ㄥ娑插姞鍒 400 渭L PEG300 涓紝娣峰悎鍧囧寑锛涘悜涓婅堪浣撶郴涓姞鍏?0 渭L Tween-80锛屾贩鍚堝潎鍖€锛涚劧鍚庣户缁姞鍏 450 渭L鐢熺悊鐩愭按瀹氬鑷 1 mL銆侟/p>

    灏 0.9 g 姘寲閽狅紝瀹屽叏婧惰В浜 100 mL ddH2O 涓紝寰楀埌婢勬竻閫忔槑鐨勭敓鐞嗙洂姘存憾娑秉/div>
  • 3.

    璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 10% DMSO90% (20%SBE-尾-CDin saline)

    Solubility: 鈮 2.5 mg/mL (9.78 mM); Clear solution

    姝ゆ柟妗堝彲鑾峰緱 鈮 2.5 mg/mL (9.78 mM锛岄ケ鍜屽害鏈煡) 鐨勬緞娓呮憾娑层€侟/p>

    浠 1 mL 宸ヤ綔娑蹭负渚嬶紝鍙 100 渭L 25.0 mg/mL 鐨勬緞娓 DMSO 鍌ㄥ娑插姞鍒 900 渭L20% 鐨 SBE-尾-CD 鐢熺悊鐩愭按姘存憾娑秉/span>涓紝娣峰悎鍧囧寑銆侟/p>

    灏 2 g 纾轰竵鍩洪啔 尾-鐜硦绮惧姞鍏 5 mL 鐢熺悊鐩愭按涓紝鍐嶇敤鐢熺悊鐩愭按瀹氬鑷 10 mL锛屽畬鍏ㄦ憾瑙ｏ紝婢勬竻閫忔槑
  • 4.

    璇蜂緷搴忔坊鍔犳瘡绉嶆憾鍓傦細 10% DMSO90%corn oil

    Solubility: 鈮 2.5 mg/mL (9.78 mM); Clear solution

    姝ゆ柟妗堝彲鑾峰緱 鈮 2.5 mg/mL (9.78 mM锛岄ケ鍜屽害鏈煡) 鐨勬緞娓呮憾娑诧紝姝ゆ柟妗堜笉閫傜敤浜庡疄楠屽懆鏈熷湪鍗婁釜鏈堜互涓婄殑瀹為獙銆侟/p>

    浠 1 mL 宸ヤ綔娑蹭负渚嬶紝鍙 100 渭L 25.0 mg/mL 鐨勬緞娓 DMSO 鍌ㄥ娑插姞鍒 900 渭L鐜夌背娌逛腑锛屾贩鍚堝潎鍖€銆侟/p>

*浠ヤ笂鎵€鏈夊姪婧跺墏閮藉彲鍦ㄦ湰缃戠珯閫夎喘銆侟/span>
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