| Bioactivity | Ditolylguanidine (1,3-Di-o-tolylguanidine) is an agonist of sigma receptor (σ1/σ2 receptor) with Ki values of 69 and 21 nM for σ1 and σ2 receptors, respectively. Ditolylguanidine effectively inhibits the growth of small cell lung cancer cells. Ditolylguanidine can be used for the research of lung cancer[1][2][3][4]. | ||||||||||||
| Invitro | Ditolylguanidine (39-60 nM) 剂量依赖性地抑制 N-(2-piperidinoethyl)4-iodobenzamide) (IPAB)， Ki 值为 40 nM[2]。Ditolylguanidine 抑制小细胞肺癌细胞株 NCI-N417 和 NCI-H209, IC50 值分别为 100 和 90 nM[3]。Ditolylguanidine (0-10 μM) 对 σ1 和 σ2 受体的 Ki 值分别为 69 和 21 nM[4]。 | ||||||||||||
| In Vivo | Ditolylguanidine (静脉注射；1-5 mg/kg，一次) 影响麻醉大鼠排尿间隔和阈压[1]。Ditolylguanidine (脑室内给药；1 μg，一次) 延长排尿间隔时间，提高麻醉大鼠的阈值压力[1]。 Animal Model: | ||||||||||||
| Name | Ditolylguanidine | ||||||||||||
| CAS | 97-39-2 | ||||||||||||
| Formula | C15H17N3 | ||||||||||||
| Molar Mass | 239.32 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Shimizu I, et al. Effects of (+)-pentazocine and 1,3-di-o-tolylguanidine (DTG), sigma (sigma) ligands, on micturition in anaesthetized rats. Br J Pharmacol. 2000 Oct;131(3):610-6. [2]. John CS, et al. Sigma receptors are expressed in human non-small cell lung carcinoma. Life Sci. 1995;56(26):2385-92. [3]. Moody TW, et al. Sigma ligands inhibit the growth of small cell lung cancer cells. Life Sci. 2000 Apr 7;66(20):1979-86. [4]. Moison D, et al. Intrastriatal administration of sigma ligands inhibits basal dopamine release in vivo. Neuropharmacology. 2003 Dec;45(7):945-53. |