ChemInform Abstract: BASIC ETHERS OF CYCLOHEXYLPHENOLS WITH β‐BLOCKING ACTIVITY. SYNTHESIS AND PHARMACOLOGICAL STUDY OF EXAPROLOL

Carissimi, M; Gentili, Patrizia; Grumelli, E; Milla, E; Picciola, G.; Ravenna, F

doi:10.1002/chin.197629170

Cited by 3 publications

(1 citation statement)

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“…The sixth group, cyclohexylphenols, were developed by Pfizer during the 1970’s and 1980’s (Carissimi et al, 1976). The classical cannabinoids (seventh group) is the oldest; synthesis began in the 1960’s following the identification of the chemical structure of THC (Mechoulam and Gaoni, 1965, 1967; Gaoni and Mechoulam, 1971).…”

Section: Synthetic Cannabinoid Agonistsmentioning

confidence: 99%

Cannabinoid Receptor 2: Potential Role in Immunomodulation and Neuroinflammation

Rom

Persidsky

2013

J Neuroimmune Pharmacol

199

121

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An accumulating body of evidence suggests that endocannabinoids and cannabinoid receptors type 1 and 2 (CB1, CB2) play a significant role in physiologic and pathologic processes, including cognitive and immune functions. While the addictive properties of marijuana, an extract from the Cannabis plant, are well recognized, there is growing appreciation of the therapeutic potential of cannabinoids in multiple pathologic conditions involving chronic inflammation (inflammatory bowel disease, arthritis, autoimmune disorders, multiple sclerosis, HIV-1 infection, stroke, Alzheimer’s disease to name a few), mainly mediated by CB2 activation. Development of CB2 agonists as therapeutic agents has been hampered by the complexity of their intracellular signaling, relative paucity of highly selective compounds and insufficient data regarding end effects in the target cells and organs. This review attempts to summarize recent advances in studies of CB2 activation in the setting of neuroinflammation, immunomodulation and HIV-1 infection.

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Section: Synthetic Cannabinoid Agonistsmentioning

confidence: 99%

Cannabinoid Receptor 2: Potential Role in Immunomodulation and Neuroinflammation

Rom

Persidsky

2013

J Neuroimmune Pharmacol

199

121

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Tissue distribution of exaprolol in rat

Faberová

Trnovec

Zemánek

et al. 1985

European Journal of Drug Metabolism and Pharmacokinetics

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The disposition of the beta adrenoceptor blocking drug 1-(2-cyclohexylphenoxy)-3-isopropylamino-2-propanol, exaprolol, in organs of the rat has been studied. After i.v. administration of 3H-exaprolol a transient extremely high accumulation of the drug in lungs was observed with a peak of 7.7% of dose/g 30 min post-administration. The disposition pattern in heart, kidneys and liver may be characterized by a tissue to plasma ratio about ten. Lower exaprolol tissue levels were observed after oral administration. The tissue to plasma ratios showed an initial increase followed by constant levels. The distribution of exaprolol in organs of the rat is discussed in the light of the previously determined pharmacokinetic parameters.

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The effect of exaprolol (MG 8823) on epicardial ST‐segment changes in a feline model of acute myocardial ischaemia

Parratt

Udvary

1983

British J Pharmacology

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3 Exaprolol (1.0mg kg-, intravenously) a potent P-adrenoceptor blocking agent with 'membrane stabilising activity', when given 1 h after the onset of ischaemia, reduced heart rate and LV dP/dt,, and increased LVEDP. These effects were prolonged (i.e. little recovery in heart rate 3 h after administration). 4 Exaprolol decreased total ST-segment elevation immediately after administration; this was significantly different from the effect of intravenous saline and lasted for at least 3 h. The effects appeared to be greater at sites of less pronounced ischaemia. 5 Intramyocardial temperature records were taken to indicate a reduction in blood flow to the ischaemic region; however the alleviation of epicardial ST-segment elevation suggests an improved myocardial oxygen demand: supply ratio. 6 Reperfusion was unsuccessfully attempted after a 4 h occlusion period; reperfusion after a shorter period (30 min) resulted in ventricular ectopic activity but no fibrillation.

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ChemInform Abstract: BASIC ETHERS OF CYCLOHEXYLPHENOLS WITH β‐BLOCKING ACTIVITY. SYNTHESIS AND PHARMACOLOGICAL STUDY OF EXAPROLOL

Abstract: Die Darstellung der Verbindungen der allgemeinen Formel (I) wird beschrieben und die pharmakologische Aktivität speziell von Exaprolol (R1= Cyclohexyl, R2=H) geprüft.

Cited by 3 publications

References 0 publications

Cannabinoid Receptor 2: Potential Role in Immunomodulation and Neuroinflammation

Cannabinoid Receptor 2: Potential Role in Immunomodulation and Neuroinflammation

Tissue distribution of exaprolol in rat

The effect of exaprolol (MG 8823) on epicardial ST‐segment changes in a feline model of acute myocardial ischaemia

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