神经肽DGAVP和Org2766对神经细胞内游离Ca2+的影响

运用Ca²⁺指示剂Fura-2作为细胞内钙离子的荧光探针,利用AR—CM—MIC阳离子测定系统,检测了分离的神经细胞内游离钙及其变化,并观测了DGAVP和Org2766对蛋白质合成抑制剂茴香霉素(ANI)引起细胞内钙离子浓度([Ca²⁺]_i)变化的影响。结果表明茴香霉素可使[Ca²⁺]_i显著升高,且有量效关系;DGAVP本身并不引起[Ca²⁺]_i发生显著变化,但适当剂量的DGAVP可显著对抗一定剂量范围内ANI升高[Ca²⁺]_i的作用,提示DGAVP对抗ANI的蛋白质合成抑制效应可能是通过拮抗ANI升高[Ca²⁺]_i这一途径实现的,另一神经肽Org2766则可能不是通过这一机制发生作用。从细胞内Ca²⁺的角度看,这两种肽的作用机理显然是不同的。     

The effect of Yohimbine, an alpha2 adrenergic receptor antagonist, on the growth hormone response to apomorphine in normal subjects.

Yohimbine HCl (16 mg po) administered 30 min before clonidine (CLON) (2 ug/kg infused over 10 min) (N = 5) or apomorphine HCl (Apo) (0.5 mg sc) (N = 10) antagonized the growth hormone (GH) response to CLON but had no effect on the GH response to Apo in normal men. This finding suggests that in humans, alpha2 adrenergic mechanisms do not modulate dopaminergic function, at least not in the hypothalamic-pituitary axis, and that the GH response to Apo is not mediated via an alpha2 adrenergic link.     

6-(αα-二苯基乙酰哌嗪基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮对兔血小板聚集及TXB2,cAMP的影响

6-(αα-二苯基乙酰哌嗪基苯基)-4,5-二氢-5-甲基-3(2H)-哒嗪酮(简称DMDP)是我院新合成的哒嗪酮的衍生物。DMDP可以显著抑制由花生四烯酸(AA(?),ADP和血小板活化因子(PAF)诱导的免血小板聚集,其IC₅₀分别为1.12±0.1.4.19±0.5和2.97±0.1μmol/L。实验还表明DMDP在1～500 μmol/L浓度范围内呈剂量依赖性地抑制兔血小板内血栓素B₂含量,但升高兔血小板内环腺苷酸水平,这可能是其抑制血小板聚集的作用机理之一。     

钙拮抗剂TMB-8抑制BHQ,NE和KCl引起的培养乳牛基底动脉单个平滑肌细胞内游离钙的升高

用ＡＲＣＭＭＩＣ阳离子测定系统，测量单个细胞内游离钙浓度（［Ｃａ２＋］ｉ），研究８（Ｎ，Ｎ二乙胺）ｎ辛基３，４，５三甲氧基苯甲酸酯（ＴＭＢ８）对培养乳牛基底动脉平滑肌［Ｃａ２＋］ｉ的作用。在细胞外钙浓度为１３ｍｍｏｌ·Ｌ－１时，ＴＭＢ８（３０μｍｏｌ·Ｌ－１）可明显抑制ＢＨＱ，ＮＥ及ＫＣｌ引起［Ｃａ２＋］ｉ的升高。在细胞外钙为零＋ＥＧＴＡ０１ｍｍｏｌ·Ｌ－１时，ＴＭＢ８（１０，３０及１００μｍｏｌ·Ｌ－１）可浓度依赖性地降低静息［Ｃａ２＋］ｉ，ＴＭＢ８（３０μｍｏｌ·Ｌ－１）可几乎完全阻断ＢＨＱ及ＮＥ引起［Ｃａ２＋］ｉ的增加。研究表明ＴＭＢ８降低培养乳牛基底动脉平滑肌［Ｃａ２＋］ｉ的机制，主要是抑制肌浆网Ｃａ２＋的释放，或增加肌浆网对Ｃａ２＋的摄入，并由此间接地抑制细胞外钙的内流。     

Clonidine-induced growth hormone secretion in chronic schizophrenia

Clonidine (0.15 mg intravenously), an alpha-adrenergic receptor agonist, was administered to 13 male chronic schizophrenics, who had been withdrawn from chronic neuroleptic therapy, and to 18 normal male controls. There was no significant difference in growth hormone (GH) response between the two groups. There was no significant correlation between duration of psychosis, duration of neuroleptic therapy or length of neuroleptic withdrawal and GH response. These results suggest that postsynaptic alpha-adrenergic receptor function in the hypothalamic-pituitary axis is unaltered in chronic schizophrenia or by prior chronic neuroleptic therapy.     

中药丹参有效成分——丹参酮ⅡA的新的全合成方法

中药丹参为活血化瘀药。近几十年来植化工作者从丹参中分离出许多有效成分,其中丹参酮ⅡA有较好的抗菌活性和心血管系统活性,已被制成磺酸钠盐而用于临床(丹参精注射液),对心绞痛治疗总有效率达85%。过去也曾有人进行过丹参酮ⅡA的全合成。Baillie等以7-甲氧基-1-四氢萘酮为原料经十二步反应,Kakisawa等以2,3,4-三甲氧基苯甲酰     

小檗碱对培养大鼠神经细胞内游离Ca2+的影响

以Fura-2/AM为细胞内钙离子的荧光指示剂,用AR-CM-MIC阳离子测定系统,直接测定了体外培养的新生大鼠神经细胞内游离钙([Ca²⁺]i)值,并观察了小檗碱(Ber)的影响。结果表明,Ber对神经细胞静息[Ca²⁺]i无明显影响,Ber1～100μmol·L^-1能剂量依赖地抑制去甲肾上腺素和H₂O₂引起的[Ca²⁺]i升高,其IC₅₀分别为39.9和17.9μmol·L^-1。高剂量Ber(10～100μmol·L^-1)能抑制高K+引起的[Ca²⁺]i升高。姐果提示,Ber对去甲肾上腺素,高K⁺及H₂O₂引起的[Ca²⁺]i升高的抑制作用可能是其抗脑缺血作用机制之一。     

Neuroendocrine evaluation of CCK-peptides on dopaminergic function in man

1. 1. CCK-33 (225 Ivy Dog Units iv) antagonized the growth hormone response to the dopamine receptor agonist, apomorphine HCl (0.5 mg sc), and increased basal prolactin secretion in normal male volunteers. A stress mediated prolactin effect could not be excluded.

2. 2. CCK-8 (5 ug iv) antagonized the growth hormone response to apomorphine but had no effect on basal prolactin or plasma homovanillic acid.

3. 3. Ceruletide (0.3 ug/kg im) had no effect on basal prolactin or apomorphine-induced growth hormone secretion.

4. 4. CCK-33, CCK-8 and ceruletide had no effect on basal growth hormone secretion which suggests that they do not inhibit the release of growth hormone.

5. 5. These findings are compatible with an inhibitory effect of CCK-33 and CCK-8 (or fragments) on dopaminergic function in man, at least in the hypothalamic-pituitary axis and point to a simple way to study the effect of peptides on dopaminergic function in man including those which may not cross the blood brain barrier.

Hello,can you hear me? Orthopaedic clinic telephone consultations in the COVID-19 era- a patient and clinician perspective

BACKGROUNDThe coronavirus disease 2019 (COVID-19) pandemic has resulted in seismic changes in healthcare delivery. As a result of this, hospital footfall required to be reduced due to increased risk of transmission of infection. To ensure patients can safely access healthcare, we introduced orthopaedic clinic telephone consultations in our busy district general hospital.AIMTo investigate patients’ and clinicians’ perspective of telephone consultations during COVID-19, and whether this method of consultation could be a viable option in the post- pandemic future. METHODSThis is a single centre, prospective study conducted in a busy National Health Service district general hospital. In May 2020, 100 non- consecutive adult patients were contacted by independent investigators within 48 h of their orthopaedic clinic telephone consultation to complete a telephone satisfaction questionnaire. The questions assessed satisfaction regarding various aspects of the consultation including overall satisfaction and willingness to use this approach long term. Satisfaction and perspective of 25 clinicians conducting these telephone consultations was also assessed via an online survey tool.RESULTS93% of patients were overall satisfied with telephone consultations and 79% were willing to continue this method of consultation post- pandemic. Patients found telephone consultations to reduce personal cost and inconvenience associated with attending a hospital appointment. 72% of clinicians reported overall satisfaction with this service and 80% agreed that telephone consultations should be used in the future. The majority found it less laborious in time and administration in comparison to face to face consultations. Patients and clinicians expressed their desire for video consultations as a method of further improving their experience with remote consultations.CONCLUSIONOur study has shown that telephone consultations are a safe and rapid method of adaptation to the COVID-19 pandemic, achieving the aim of reducing hospital footfall. This method of consultation has resulted in immense clinician and patient satisfaction. Our findings suggest that this tool has benefits in post pandemic healthcare delivery. It has also highlighted that telephone consultations can act as a steppingstone to the introduction of the more complex platform of video consulting.     

丁公藤碱Ⅱ类似物的合成及其生物活性

本文设计合成了丁公藤碱Ⅱ的C₂脱氧和C₈电子等排类似物。药理结果表明,丁公藤碱Ⅱ的C₂羟基是保持其缩瞳活性的关键部分之一;目的物2和4各自分别具有拟和抗胆碱活性;电子等排目的物16和17既无拟也无抗胆碱作用。