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At least 199 records · Page 11Linked to original sources
PubMed1990

Brain protection: physiological and pharmacological considerations. Part II: The pharmacology of brain protection.

Neuroprotective agents may exert their effect by reducing cerebral oxygen demand (CMRO2), increasing cerebral oxygen delivery, or by altering ongoing pathological processes. Barbiturates provide neuroprotection by reducing the CMRO2 necessary for synaptic transmission while leaving the component necessary for cellular metabolism intact. Isoflurane may exert a neuroprotective effect by a similar mechanism but its efficacy is likely less than that of barbiturates due to adverse effects on cerebral blood flow. Lidocaine reduces CMRO2 by affecting both cellular metabolic processes and synaptic transmission and thus resembles hypothermia in its mechanism of action. Benzodiazepines reduce CMRO2 by reducing synaptic transmission and their use as neuroprotectants produces less haemodynamic compromise than barbiturates. The mechanism of protection by calcium entry blocking agents appears to be due to improved blood flow as opposed to altering abnormal Ca++ fluxes. In contrast, agents such as ketamine and MK-801 may prevent abnormal Ca++ fluxes through their competitive interaction with N-methyl-D-aspartate receptors. Phenytoin prevents K(+)-mediated ischaemic events from progressing. Agents worthy of further investigation include corticosteroids, free radical scavengers, prostaglandin inhibitors and iron chelators.

Anesthetics↗
PubMed2002

SPASE-I: a multicenter observational study on pharmacological treatment of acute stroke in the elderly. The Italian Study of Pharmacological Treatment of Acute Stroke in the Elderly Group.

We investigated the clinical outcome and current therapeutic management of ischemic stroke in elderly patients in different neurological wards throughout Italy. Twelve centers in 10 Italian regions were involved. The clinical and instrumental data were prospectively collected for 335 patients 65 years or older, presenting in a 12-months period. At the multivariate analysis, death was associated with the presence of total anterior circulation infarct and the use of antiedema agents. Stroke-related disability was related to female sex, unified stroke scale (USS) scores at entry and mini-mental state examination (MMSE) scores at the 1-months follow-up. The majority of patients (70%) received antiplatelets to prevent stroke recurrence. Very elderly (> or =80 years) patients had worse presentation and prognosis than less elderly stroke victims (<80 years). Age played an important role in the therapeutic approach to stroke: while antiplatelets were widely used, oral anticoagulants were underused even when specifically indicated.

Age Factors↗
PubMed1995

Behavioural pharmacology of 'D-1-like' dopamine receptors: further subtyping, new pharmacological probes and interactions with 'D-2-like' receptors.

1. D-1 receptors are now recognised to play a critical psychopharmacological role in the regulation of unconditioned motor and numerous other aspects of behaviour. 2. There appears to exist a broad family of 'D-1-like' receptors in terms both of differential coupling to distinct messenger/transduction mechanisms and of gene cloning, whose behavioural roles remain to be clarified. 3. The adenylyl cyclase-inhibiting benzazepine SK&F 83959 induces behavioural responses in rats that are similar to those induced by the full efficacy cyclase-stimulating isochroman A 68930 but not to those induced by its high efficacy partial agonist benzazepine congener R-6-Br-APB; these data indicate roles for individual 'D-1-like' receptors in mediating distinct elements of dopaminergic behaviour. 4. The putative D-1 autoreceptor agonist B-HT 920 and the putative D-3 agonist 7-OH-DPAT demonstrate different behavioural profiles when given both alone and in combination with the selective 'D-1-like' antagonist BW 737C; D-3 receptors may participate in cooperative/synergistic but not in oppositional 'D-1-like': 'D-2-like' interactions. 5. Such interactions apparent at the level of behaviour are complemented by evidence for similar interactions at numerous alternative levels of function, though these may differ between rodent and primate species. 6. A broader range of more selective agonists and antagonists, able to distinguish between individual members of the 'D-1-like' and of the 'D-2-like' receptor families are needed to clarify these issues.

Animals↗
PubMed2005

Pharmacology of gap junctions. New pharmacological targets for treatment of arrhythmia, seizure and cancer?

Intercellular communication in many organs is maintained via intercellular gap junction channels composed of connexins, a large protein family with a number of isoforms. This gap junction intercellular communication (GJIC) allows the propagation of action potentials (e.g., in brain, heart), and the transfer of small molecules which may regulate cell growth, differentiation and function. The latter has been shown to be involved in cancer growth: reduced GJIC often is associated with increased tumor growth or with de-differentiation processes. Disturbances of GJIC in the heart can cause arrhythmia, while in brain electrical activity during seizures seems to be propagated via gap junction channels. Many diseases or pathophysiological conditions seem to be associated with alterations of gap junction protein expression. Thus, depending on the target disease opening or closure of gap junctions may be of interest, or alteration of connexin expression. GJIC can be affected acutely by changing gap junction conductance or--more chronic--by altering connexin expression and membrane localisation. This review gives an overview on drugs affecting GJIC.

Animals↗
PubMed2001

Synthesis and pharmacological activity of new carbonyl derivatives of 1-aryl-2-iminoimidazolidine. Part 1. Synthesis and pharmacological activity of chain derivatives of 1-aryl-2-iminoimidazolidine containing urea moiety.

The synthesis and physicochemical properties of new carbonyl derivatives of 1-aryl-2-iminoimidazolidine are presented. Isomeric 1-(1-arylimidazolidine-2-ylidene)-3-arylureas (series A) and 1-aryl-2-imine-3-arylaminocarbonylimidazolidines (series B) were obtained after the condensation reaction of 1-aryl-2-iminoimidazolidines and arylisocyanates. 1-Aryl-2-iminoimidazolidines were synthesised in a two-step reaction from the respective anilines. The molecular structure of 1-(1-phenylimidazolidine-2-ylidene)-3-(4-chlorophenyl)urea (A2) has been determined by X-ray crystallography. The representatives of both investigated series were evaluated in behavioural animal tests. They exhibited significant, especially analgesic, activity on the animal central nervous system (CNS). They displayed substantial effect on the serotonine and catecholamine neurotransmission as well, at very low toxicity (LD(50) over 2000 mg kg(-1) i.p.). In the binding affinity tests they exhibited moderate affinity (on the micromolar level) toward opioid (mu) and serotonine (5HT(2)) receptors. The derivatives of series A had moderate affinity toward benzodiazepine (BZD) receptor as well. Distinctive differences observed in their activity spectra can be connected with the presence of particular structural features such as relative orientation of the two aromatic rings and the carbonyl moiety.

Analgesics↗
PubMed1998

Moxonidine: pharmacology, clinical pharmacology and clinical profile.

Management strategies in hypertension evolve in response to an increased understanding of underlying pathophysiological processes and developments and refinements in drug treatments. Recent research has identified the regulatory role of the imidazoline (I1) receptor in sympathetic outflow and blood pressure regulation and this has led to the development of moxonidine, a highly selective centrally acting antihypertensive agent. At a practical level, moxonidine is suitable for single daily dosing in hypertension. Furthermore, in comparative studies moxonidine has a low incidence of symptomatic adverse effects comparable, for example, to that of the ACE inhibitor drugs, captopril and enalapril. The antihypertensive efficacy of moxonidine has now been established in a series of comparative clinical trials against all other first-line antihypertensive drug classes but, in line with current concepts, it may be necessary to look beyond blood pressure reduction. For example, centrally acting agents are known to be effective for promoting the regression of LV hypertrophy and studies in hypertensive patients have shown that antihypertensive treatment with moxonidine successfully leads to significant reductions in LV mass indices. Furthermore, there is now evidence that moxonidine has a beneficial effect on insulin sensitivity such that there are likely to be improvements in the overall metabolic profile. Thus, the clinical characteristics of moxonidine indicate that it is well suited for consideration among the first-line antihypertensive treatment choices.

Antihypertensive Agents↗