阿帕替尼联合NP化疗治疗晚期非小细胞肺癌疗效及对患者血清肿瘤标志物和生存质量的影响

摘 要 目的：探讨阿帕替尼联合NP化疗治疗晚期非小细胞肺癌疗效及对患者血清肿瘤标志物和生存质量影响。 方法: 晚期非小细胞肺癌患者113例随机分为观察组57例与对照组56例。对照组患者采用NP化疗方案治疗,观察组在对照组基础上加用阿帕替尼治疗。两组疗程均为4个化疗周期,每个周期28 d。比较两组近期疗效、生活质量改善和不良反应发生情况,及治疗前后血清肿瘤标志物变化。 结果: 观察组总有效率为56.14%,生存质量提高率为71.93%,均明显高于对照组（P<0.05）。两组治疗后血清癌抗原125（CA125）、癌胚抗原（CEA）和细胞角蛋白19片段（CYFRA21 1）水平均较治疗前明显降低（P<0.05）,且观察组低于对照组（P<0.05）。两组不良反应发生率差异无统计学意义（P>0.05）。 结论: 晚期非小细胞肺癌患者应用阿帕替尼联合NP化疗治疗疗效明显,且可降低血清肿瘤标志物CA125、CEA和CYFRA21 1水平及提高患者生存质量,值得临床借鉴。     

紫杉醇脂质体与紫杉醇分别联合卡铂治疗卵巢癌疗效的Meta分析

摘 要 目的：系统评价紫杉醇脂质体与普通紫杉醇制剂分别联合卡铂治疗卵巢癌的有效性和安全性。方法: 计算机检索中国知识资源总库（CNKI）、中国生物医学文献数据库（CBM）、中文科技期刊数据库（VIP）、中国学术期刊数据库（万方数据）、PubMed、Cochrane Library、Embase 中紫杉醇脂质体联合卡铂与紫杉醇联合卡铂化疗治疗卵巢癌的临床随机对照试验,检索范围均为建库至2017年7月12日。2名研究者根据Cochrane系统评价手册5.1.0,按纳入与排除标准独立进行文献筛选、资料提取、质量评价,并使用RevMan5.3软件Meta分析。 结果:共纳入8篇随机对照试验,共计793例受试者。结果显示,在卵巢癌的治疗中,紫杉醇脂质体联合卡铂与紫杉醇联合卡铂比较,客观缓解率有统计学意义（P=0.02）。在不良反应方面,紫杉醇脂质体联合卡铂与紫杉醇联合卡铂比较：血小板减少（P=0.02）、恶心呕吐（P＜0.000 01）、肌肉关节痛（P＜0.000 01）、皮疹（P＜0.000 01）、呼吸困难（P=0.000 8）和面部潮红（P=0.001 0）,差异有统计学意义;而白细胞减少（P=0.13）、血红蛋白减少（P=0.28）、腹泻便秘（P=0.15）、脱发（P=0.62）,差异无统计学意义。结论:紫杉醇脂质体联合卡铂化疗治疗卵巢癌的疗效优于紫杉醇联合卡铂化疗,且能减轻患者不良反应,提高用药有效性和安全性。     

紫杉醇联合奈达铂治疗卵巢癌的Meta分析

摘 要 目的：系统评价紫杉醇联合奈达铂对卵巢癌患者进行治疗的安全性和有效性。方法：计算机检索PubMed、Cochrane Library、Embase、CNKI、WanFang Data、SinoMed数据库,搜集有关紫杉醇联合奈达铂治疗卵巢癌的随机对照试验（RCTs）。检索时限均为建库至2018年4月,由两名研究者独立筛选文献、提取资料并评价纳入研究的偏倚风险后,采用 RevMan 5.3软件进行分析。 结果：共纳入12 项研究,包括1 219 例患者。Meta分析结果显示,紫杉醇联合奈达铂治疗卵巢癌的总有效率与其他化疗方案相比,差异无统计学意义[OR=1.14,95%CI （0.88,1.48）,P=0.16],但紫杉醇联合奈达铂可提高患者1年生存率[OR=3.37,95%CI（1.47,7.71）,P=0.004]和2年生存率[OR=2.24,95%CI（1.27,3.97）,P=0.006],并且该方案显著减少了不良反应的发生率：血小板降低[OR=0.49,95%CI（0.36,0.66）,P=0.000 01]、恶心呕吐[OR=0.65,95%CI（0.47,0.89）,P=0.007]、外周神经毒性[OR=0.43,95%CI（0.28,0.67）,P=0.000 2]及肝功能损伤[OR=0.39,95%CI（0.20,0.77）,P=0.006]等不良反应的发生率。 结论：紫杉醇联合奈达铂治疗卵巢癌可延长患者1年及2年生存率且不良反应较轻,受研究数量和质量的限制,结论还需更多高质量的RCTs进行验证。     

芪防鼻敏颗粒对变应性鼻炎大鼠炎性因子表达的影响研究

摘 要 目的：观察芪防鼻敏颗粒对变应性鼻炎（AR）大鼠血清白介素 4(IL 4),白介素 17(IL 17）,肿瘤坏死因子（TNF α）及鼻黏膜γ干扰素（IFN γ）、白介素 6（IL 6）、TNF α表达的影响。方法: SD大鼠随机分为正常组,模型组,氯雷他定组（1.17 mg·kg^-1）,鼻炎康组（0.6 g·kg^-1）,芪防鼻敏颗粒高（26.48 g·kg^-1）、中（13.24 g·kg^-1）、低（6.62 g·kg^-1）剂量组。采用卵蛋白（OVA）建立AR大鼠模型。造模成功后分别灌胃给药,连续14 d。酶联免疫吸附法（ELISA）检测AR大鼠血清IL 4、IL 17、TNF α水平,免疫组化染色法（IHC）检测鼻黏膜IFN γ、IL 6、TNF α表达。结果:与正常组相比,模型组大鼠血清IL 4、IL 17水平明显上升（P<0.01）;鼻黏膜IFN γ阳性表达明显降低（P<0.05）,IL 6、TNF α阳性表达显著升高（P<0.01）。与模型组相比,氯雷他定组、芪防鼻敏颗粒中剂量组大鼠血清IL 4水平显著下降（P<0.05）,芪防鼻敏颗粒低剂量组大鼠血清IL 17水平明显下降（P<0.05）,氯雷他定组、鼻炎康组、芪防鼻敏颗粒高、中剂量组大鼠血清TNF α水平显著下降（P<0.05或P<0.01）;高、低剂量组大鼠鼻黏膜IFN γ阳性表达显著升高（P<0.05或P<0.01）,高、中剂量组IL 6阳性表达显著降低（P<0.01）,高剂量组TNF α阳性表达显著降低（P<0.01）。与氯雷他定组相比,鼻炎康组、芪防鼻敏颗粒高剂量组大鼠血清IL 17水平明显上升（P<0.05）,鼻炎康组、芪防鼻敏颗粒低剂量组大鼠血清IL 4水平明显上升（P<0.05）,芪防鼻敏颗粒高、中、低剂量组TNF α阳性表达显著升高（P<0.05）;与鼻炎康组比较,芪防鼻敏颗粒中剂量组大鼠血清IL 4水平明显下降（P<0.05）;与芪防鼻敏颗粒低剂量组相比,芪防鼻敏颗粒高剂量组大鼠血清IL 17水平明显上升（P<0.05）,芪防鼻敏颗粒中剂量组大鼠血清IL 4水平明显下降（P<0.05）。结论:芪防鼻敏颗粒可增加AR鼻黏膜IFN γ表达,降低血清IL 4、TNF α、IL 17水平及鼻黏膜TNF α、IL 6表达。     

晚期非小细胞肺癌患者XPG基因多态性与铂类药物化疗敏感性的Meta分析

摘 要 目的：用Meta分析方法对晚期非小细胞肺癌（NSCLC）患者核苷酸切除修复基因XPG/ERCC5单核苷酸多态性与铂类药物化疗敏感性的相关性进行分析。方法：在PubMed、Cochrabe Libray、 Embase数据库和中国生物医学文献数据库（SinoMed）、中国学术期刊全文数据库（CNKI）、中文科技期刊全文数据库维普（VIP）、万方数据库中检索有关晚期NSCLC患者XPG/ERCC5基因46位点[XPG His46His]基因多态性与应用铂类药物化疗疗效相关性的研究,对符合标准的研究进行资料提取,采用Cochrane系统评价员手册5.1.0进行方法学质量评价,采用 RevMan 5.3软件进行Meta分析。结果：共纳入6项研究,合计983例患者。基因检测结果发现XPG His46His基因多态性分为变异型基因型C/T、T/T和野生型基因型C/C。Meta分析结果显示,晚期NSCLC患者携带XPG His46His基因中T/T基因型的化疗敏感性明显低于C/C基因型,差异有统计学意义（OR=0.40,95%CI：0.24~0.65,P=0.000 3）;而携带C/T基因型的化疗敏感性与C/C基因型比较差异无统计学意义（OR=0.80,95%CI：0.55~1.16,P=0.23）;携带变异型基因型C/T+T/T与野生型基因型C/C比较,携带变异型基因型的患者化疗敏感性低于野生型基因型C/C,差异有统计学意义（OR=0.56,95%CI：0.41~0.75,P=0.000 1）。另外亚组分析显示,病理分期为Ⅳ期的XPG His46His基因变异型与野生型相比,携带变异型C/T+T/T患者较野生型C/C对化疗敏感性降低,差异有统计学意义（OR=0.40,95%CI：0.20~0.82,P=0.01）。结论：晚期NSCLC核苷酸切除修复基因XPG/ERCC5野生型基因型C/C携带者对铂类化疗敏感性优于携带变异型基因型C/T+T/T、T/T的患者。但是由于纳入的研究数量较少,随着更多临床研究的开展,结论需要进一步验证。     

活犀角与犀角抗炎作用的比较研究

摘 要 目的：比较活犀角与犀角的抗炎作用有无显著差异,为活犀角替代犀角提供实验依据。 方法: 通过大鼠足跖肿胀法和小鼠棉球肉芽肿法、耳廓肿胀法、腹腔染料通透法研究活犀角和犀角的抗炎作用。 结果: 与模型对照组比较,活犀角的高（440 mg·kg^-1）、中（220 mg·kg^-1）剂量组和犀角3个剂量组各时间点的足跖肿胀度差异有统计学意义（P＜0.05或P＜0.01）;活犀角和犀角的高（700 mg·kg^-1）、中（350 mg·kg^-1）剂量组能显著降低小鼠棉球肉芽肿的重量（P＜0.05）;活犀角和犀角3个剂量组（700,350,175 mg·kg^-1）均能明显降低二甲苯引起的小鼠耳廓肿胀（P＜0.05或P＜0.01）;犀角中（350 mg·kg^-1）剂量组,活犀角高（700 mg·kg^-1）、中（350 mg·kg^-1）剂量组的腹腔清洗液中伊文思兰的吸光度值显著降低（P＜0.05或P＜0.01）。活犀角与犀角相同剂量组间抗炎作用比较无显著差异。 结论: 活犀角与犀角均具有一定抗炎作用,本研究为活犀角在抗炎作用方面作为犀角的替代品进行使用提供了实验依据。     

三七总皂苷肠溶微丸对高脂血症家兔血液流变学的影响

摘 要 目的：探讨三七总皂苷（PNS）肠溶微丸对家兔血液流变学的影响。方法: 建立空白对照组、模型组、血栓通注射剂（冻干）组（15 mg·kg^-1·d^-1,im）、PNS肠溶微丸高剂量组（45 mg·kg^-1·d^-1,ig）、中剂量组（30 mg·kg^-1·d^-1,ig）、低剂量组（15 mg·kg^-1·d^-1,ig）,予高脂饲料配方灌胃造模;运用血液流变学检测方法测定各组全血黏度、血浆黏度 、红细胞聚集指数、红细胞刚性指数、红细胞电泳率5项指标。结果: 模型组血液流变学5项指标明显高于空白对照组(P<0.01),提示动物模型复制成功。与模型组比较, PNS肠溶微丸高、中剂量组均能明显降低全血黏度和血浆黏度（P<0.01或P<0.05）;PNS肠溶微丸低剂量组能显著降低中切黏度及血浆黏度（P<0.05）;PNS肠溶微丸高、中、低剂量组红细胞聚集指数显著降低（P<0.01）;PNS肠溶微丸高、中剂量组红细胞刚性指数显著降低（P<0.01或P<0.05）;PNS肠溶微丸高、中、低剂量有降低红细胞电泳率的趋势,但差异无统计学意义（P>0.05）。PNS肠溶微丸中剂量组降低中切黏度效果优于血栓通注射剂（冻干）组（P<0.05）。结论:PNS肠溶微丸能降低家兔全血黏度、血浆黏度、红细胞聚集指数、红细胞刚性指数、红细胞电泳率等指标,发挥PNS肠溶微丸活血化瘀、抑制血栓形成、增加心脑血管的血液供应的作用。     

苦参素胶囊对BALB/c小鼠人肝癌细胞株SMMC 7721体外种植瘤的影响

摘 要 目的：观察苦参素胶囊对BALB/c小鼠人肝癌细胞株SMMC 7721体外种植瘤的影响。方法: 采用体外传代培养人肝癌SMMC 7721细胞株,建立体外种植瘤小鼠肝癌模型。随机分为模型组、氟尿嘧啶（5 Fu）组（25 mg·kg^-1）、苦参素胶囊高剂量组（90 mg·kg^-1）、苦参素胶囊低剂量组（45 mg·kg^-1）,另设空白对照组。每组10只,连续给药14 d后。眼球取血,分离血清,Elisa法测定IL 2水平。摘取瘤株,称量湿质量,计算抑制率;HE染色,观察肿瘤组织的病理改变。结果: 与模型组比较,苦参素胶囊高、低剂量组可显著升高小鼠血清IL 2含量（P<0.01或P<0.05）;抑制体外种植瘤生长（P<0.001或P<0.05）;高剂量组上述作用与5 Fu组相比无明显差异（P>0.05）。HE染色可见小鼠肿瘤细胞核染色变浅,肿瘤细胞数量减少。结论: 苦参素胶囊对BALB/c小鼠人肝癌细胞株体外种植瘤有一定的抑制作用。     

百令胶囊对腹膜透析患者腹透液中间皮细胞转化生长因子β1水平的影响

摘 要 目的： 观察百令胶囊对腹膜透析患者腹透液中间皮细胞转化生长因子β1（TGF-β1）水平的影响。方法: 40例行腹膜透析的患者随机分为对照组和试验组各20例,两组均应用1.5%腹膜透析液,6 000 ml·dd^-1,试验组再加用百令胶囊2.5g,po,tid,共观察6个月。1个月时评估两组透析充分性[指标：尿素清除指数（Kt/V）及内生肌酐清除率（Ccr）],比较两组患者1,3,6个月时肾功能及腹透液中TGF-β1水平变化。结果: 透析1个月时,两组Kt/V及Ccr比较无差异,血肌酐均明显降低（P＜0.05）,3,6个月两组血肌酐水平无明显波动。对照组1,3,6个月TGF β1水平逐渐升高（P＜0.05）,试验组TGF β1水平无明显变化（P＞0.05）,且明显低于对照组（P＜0.05）。结论:口服百令胶囊可降低患者腹透液中TGF β1水平,从而抑制腹膜纤维化的发展。     

HPLC波长切换法同时测定茵栀祛黄胶囊中7种成分的含量

摘 要 目的：建立HPLC波长切换法同时测定茵栀祛黄胶囊中栀子苷、甘草苷、芦荟大黄素、大黄酸、大黄素、大黄酚和大黄素甲醚的含量。方法: 采用Waters Sunfire C18（250 mm×4.6 mm,5 μm）色谱柱;流动相：甲醇（A） 0.05%磷酸溶液（B）（梯度洗脱）,流速为1.0 ml·min^-1 ,柱温为25℃,检测波长(0~15 min：在238 nm波长下检测栀子苷和甘草苷;15~50 min：在254 nm波长下检测芦荟大黄素、大黄酸、大黄素、大黄酚和大黄素甲醚),进样量为10 μl。结果: 栀子苷、甘草苷、芦荟大黄素、大黄酸、大黄素、大黄酚和大黄素甲醚的线性范围分别为0.13～3.18 μg·ml^-1（r=0.999 8）、0.19～4.84 μg·ml^-1（r=0.999 7）、0.28～7.02 μg·ml^-1（r=0.999 9）、0.13～3.16 μg·ml^-1（r=0.999 9）、0.61～15.27 μg·ml^-1（r=0.999 9）、0.32～8.03 μg·ml^-1（r=0.999 9）、0.39～9.81 μg·ml^-1（r=0.999 9）;平均加样回收率分别为98.84%（RSD=0.74%）、99.34%（RSD=0.86%）、99.54%（RSD=0.30%）、99.56%（RSD=0.80%）、99.85%（RSD=0.41%）、99.57%（RSD=0.70%）、99.64%（RSD=0.30%）（n=9）。结论: 本文建立的HPLC含量测定方法,具有操作简便、专属性高、重复性良好、结果准确可靠的特点,可用于茵栀祛黄胶囊的质量控制。     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Aquatic Insects and Trace Metals: Bioavailability,Bioaccumulation, and Toxicity

Abstract

The uptake of metals from food and water sources by insects is thought to be additive. For a given metal, the proportions taken up from water and food will depend both on the bioavailable concentration of the metal associated with each source and the mechanism and rate by which the metal enters the insect. Attempts to correlate insect trace metal concentrations with the trophic level of insects should be made with a knowledge of the feeding relationships of the individual taxa concerned. Pathways for the uptake of essential metals, such as copper and zinc, exist at the cellular level, and other nonessential metals, such as cadmium, also appear to enter via these routes. Within cells, trace metals can be bound to proteins or stored in granules. The internal distribution of metals among body tissues is very heterogeneous, and distribution patterns tend to be both metal and taxon specific. Trace metals associated with insects can be both bound on the surface of their chitinous exoskeleton and incorporated into body tissues. The quantities of trace meals accumulated by an individual reflect the net balance between the rate of metal influx from both dissolved and particulate sources and the rate of metal efflux from the organism. The toxicity of metals has been demonstrated at all levels of biological organization: cell, tissue, individual, population, and community. Much of the literature pertaining to the toxic effects of metals on aquatic insects is based on laboratory observations and, as such, it is difficult to extrapolate the data to insects in nature. The few experimental studies in nature suggest that trace metal contaminants can affect both the distribution and the abundance of aquatic insects. Insects have a largely unexploited potential as biomonitors of metal contamination in nature. A better understanding of the physico-chemical and biological mechanisms mediating trace metal bioavailability and exchange will facilitate the development of general predictive models relating trace metal concentrations in insects to those in their environment. Such models will facilitate the use of insects as contaminant biomonitors.     

Pharmacological treatment of COVID-19: an opinion paper

The precocity and efficacy of the vaccines developed so far against COVID-19 has been the most significant and saving advance against the pandemic. The development of vaccines has not prevented, during the whole period of the pandemic, the constant search for therapeutic medicines, both among existing drugs with different indications and in the development of new drugs. The Scientific Committee of the COVID-19 of the Illustrious College of Physicians of Madrid wanted to offer an early, simplified and critical approach to these new drugs, to new developments in immunotherapy and to what has been learned from the immune response modulators already known and which have proven effective against the virus, in order to help understand the current situation.     

Steroidal sapogenin contents in some domestic plants

In order to find out the values of the steroid resources for the future use. the compositions and contents of steroidal sapogenins from 13 domestic plants have been investigated. As a result,Dioscorea nipponica, D. quinqueloba andSmilax china were found to have large amount of diosgenin. And pennogenin inTrillium kamtschaticum andParis verticillata, yuccagenin inAllium fistulosum, hecogenin inAgave americana and neochlorogenin inSolanum nigum were appeared to be major steroidal sapogenins.     

Alzheimer’s disease – current trends in basic and clinical research. Highlights from the 16th ECNP

Advances in the molecular biological knowledge of neuronal nicotinic acetylcholine receptors (nAChRs) have led to a growing interest by the pharmaceutical industry in the development of novel compounds that selectively modulate nAChR function. The ability of (-)-nicotine, an activator of nAChRs, to enhance attentional aspects of cognition in animals and humans, to exert neuroprotective and anxiolytic-like effects, and presumably to mediate the negative correlation between smoking and Alzheimer's (and Parkinson's) Disease, has focused interest on the potential therapeutic utility of modulators of nAChR function for treatment of some of the deficits associated with these progressive, neurodegenerative conditions. Numerous compounds are known which activate nAChRs and which might serve as lead compounds toward the development of such agents. The pharmacologic diversity of neuronal nAChR subtypes suggests the possibility of developing selective compounds which would have more favourable side-effect profiles than existing agents. This broader class of agents, collectively called cholinergic channel modulators (ChCMs), is anticipated to encompass compounds which would have more favourable side-effect profiles than existing agents, which generally exhibit low selectivity. This selectivity may be achieved by preferentially activating some subtypes of nAChRs (i.e., Cholinergic Channel Activators, ChCAs) or inhibiting the function of other subtypes (Cholinergic Channel Inhibitors, ChCIs). An overview of the biology of nAChRs and the rationale for the use of ChCMs for the treatment of dementia related to neurodegenerative diseases are presented, followed by a discussion of lead compounds and compounds under consideration for clinical evaluation.