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On the cerebral accumulation of ketamine and the relationship between metabolism of the drug and its pharmacological effects.
  • M. Cohen, A. Trevor
  • Chemistry, Medicine
    The Journal of pharmacology and experimental…
  • 1 May 1974
Determination of the partition coefficients of ketamine and its N-demethylated product (metabolite I) indicated that both compounds were highly lipid soluble which may account for their rapid accumulation by cerebral tissues.
Effects of oxidized low-density lipoprotein on vascular contraction and relaxation: clinical and pharmacological implications in atherosclerosis.
The beneficial effect of lipid-lowering therapy and the ability of antioxidants to alleviate vasomotor disturbances in hypercholesterolemia and slow the progression of atherosclerosis, strongly support a causative role of oxidized LDL in mediating vascular dysfunction in vivo and contributing to the clinical sequalae of coronary artery disease.
Distribution and Three‐Dimensional Structure of Intercellular Junctions in Canine Myocardium
True "lateral" gap junctions do not exist in working ventricular myocytes and would not likely be able to withstand shear forces created by laterally sliding cells.
Distribution in the Brain and Metabolism of Ketamine in the Rat after Intravenous Administration
Study of biotransformation in citro showed that brain tissue was incapable of metabolizing ketamine, while liver homogenates metabolized ketamine to the x-demethylated product exclusively, which accumulated in the brain.
5‐HT1F receptor agonists inhibit neurogenic dural inflammation in guinea pigs
The potency of agonists in inhibiting adenylate cyclase in cells transfected with human 5-HT1F receptor was also highly correlated with their potency in the animal model of migraine, suggesting that the 5- HT1F receptors is a rational target for migraine therapeutics.
Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.
As the first compounds reported with such selectivity and enhanced receptor affinity, these tetrahydro-beta-carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT2B receptor in normal and disease physiology.
LY215840, a high-affinity 5-HT7 receptor ligand, blocks serotonin-induced relaxation in canine coronary artery.
The ability of LY215840 to block the relaxant 5- HT receptor in canine coronary artery may reflect its 5-HT7 receptor antagonist activity and make it a useful tool to probe the relationship between the 5-Hat7 receptor and the coronary vasoactive properties of 5-ht.
Aortic valve replacement with a caged ball valve.
Pharmacological characteristics of the newly cloned rat 5-hydroxytryptamine2F receptor.
The affinity of a compound for the 5-HT2F receptor at 37 degrees versus 0 degree was shown to be useful for predicting agonist or antagonist activity, and information is provided about some of the structural requirements for the affinity of certain tryptamines at the 4-HT/1C receptor family.
Potent antagonism of 5-HT(3) and 5-HT(6) receptors by olanzapine.
Olanzapine was not an agonist, but was a potent antagonist at 5-HT(6) receptors and had marked antagonism at 5 -HT(3) receptors.