Brain, distribution

Neurotensin. This hormone has been isolated and characterized from acid—acetone extracts of bovine hypothalamus (118) on the basis of its hypotensive activity. Immunoreactive neurotensin is present in mammalian gut and is distributed throughout the central nervous system its highest concentration is in the hypothalamus and in the substantia gelatinosa of the spinal cord (119). Its overall brain distribution is not unlike that of enkephalin ( ) ... 

Norinder, U., Haeberlein, M. Computational approaches to the prediction of the blood-brain distribution. Adv. Drug Deliv. Rev. 2002, 54, 291-313. 

P., Ghlenov, M., McConnell, O., Ghait, A., Kipnis, V., Zaslavsky, B. Relative hydrophobicity and lipophilicity of drugs measured by aqueous two-phase partitioning, octanol-buffer partitioning and HPLG. A simple model for predicting blood-brain distribution. Eur. J. Med. 

Wada, H., Inagaki, N., Itowi, N. 8r Yamatodani, A. (1991). Histaminergic neuron system in the brain distribution and possible functions. Brain Res. Bull. 27, 367-70. 

S., Couet, W., In vitro and in vivo investigations on fluoroquinolones efFects of the P-glycoprotein efflux transporter on brain distribution of sparfloxadn, Eur. J. Pharm. Sci. 2000, 12, 85-93. 

In an attempt to reconcile these results, an additional investigation was carried out. This study utilized a behavioral disruption procedure, in which various doses of LSD were injected into the DRN while rats were bar pressing under a FR 10 schedule of food reinforcement (Fig. 3). As in the DS study, the DRN appeared relatively insensitive to LSD the dose required to disrupt behavior via the DRN route was 20 Mg/kg, whereas the systemic dose was 60 Mg/kg- An analysis of brain distribution data (61) would predict that LSD should have been active at a dose range of about 100 to 200 ng/kg when applied directly into the DRN neither study approached this range. 

On the basis of these results, they concluded that log Poct cannot be used to predict the blood-brain distribution rectilinearly, but could be combined with... 

Abraham MH, Chadha HS, Mitchell RC (1995) Hydrogen-bonding. Part 36. Determination of blood brain distribution using octanol-water partition coefficients. Drug Des Discov 13 123-131. 

Abraham MH, Takacs-Novak K, Mitchell RC (1997) On the partition of ampholytes application to blood-brain distribution. J Pharm Sci 86 310-315. 

Platts JA, Abraham MH, Zhao YH, Hersey A, Ijaz L, Butina D (2001) Correlation and prediction of a large blood-brain distribution data set-an LFER study. Eur J Med Chem 36 719-730. 

Wang MD, Wahlstrom G, Backstrom T. 1997. The regional brain distribution of the neurosteroids pregnenolone and pregnenolone sulfate following intravenous infusion. J Steroid Biochem Mol Biol 62(4) 299-306. 

Roselli CE, Resko JA. 2001. Cytochrome P450 aromatase CYP19) in the non-human primate brain distribution, regulation, and functional significance. J Steroid Biochem Mol Biol 79 247-253. 

Prokai L, Zharikova AD, Janaky T, Prokai-Tatrai K. 2000. Exploratory pharmacokinetics and brain distribution study of a neuropeptide FF antagonist by liquid chromatography/atmospheric pressure ionization tandem mass spectrometry. Rapid Commun Mass Spectrom 14 2412. 

Much of the data produced in studies such as this has measured the partitioning of drugs into whole brain from blood or plasma. The importance of lipophilicity in brain distribution has therefore been highlighted in many reviews [3,4], however the majority of these have concentrated on total drug concentrations which, given the lipid nature of brain tissue, over-emphasizes the accumulation of lipophilic drugs. 

Weber, S.J., Greene, D.L., Hruby, V.J., Yamamura, H I., Porreca, F., Davis, T.P. Whole body and brain distribution of fHJcyclic [D-Pen2,D-Pen 5]enkephalin after intraperitoneai, intravenous, oral and subcutaneous administration, J. Pharmacol. Exp. Ther. 1992, 263, 1308-1316. 

Thus, there were serotonin 1 receptors, and then there were 1 and 2 receptors, and then la and lb and 2a and 2b receptors, and on and on. These are called 5-HT receptors, since the chemical name for serotonin is 5-hy-droxytryptamine, and the scientist would never want to let the layman know just what he is talking about. DOI has been synthesized with a variety of radioactive iodine isotopes in it, and these tools have been of considerable value in mapping out its brain distribution. And by extrapolation, the possible localization of other psychedelic compounds that cannot be so easily labelled. A small neurochemical research company on the East Coast picked up on these properties of DOI, and offered it as a commercial item for research experiments. But I doubt that they are completely innocent of the fact that DOI is an extremely potent psychedelic and that it is still unrecognized by the Federal drug laws since, in their most recent catalog, the price had almost doubled and a note had been added to the effect that telephone orders cannot be accepted for this compound. 

Jimenez-Anguiano A, Garcia-Garcia F, Mendoza-Ramirez JL, Duran-Vazquez A, Drucker-Colin R. Brain distribution of vasoactive intestinal peptide receptors following REM sleep deprivation. Brain Res 1996 728 37-46. 

Leysen JE, Niemegeers CJ, Van Nueten JM, Laduron PM. [3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role. Mol Pharmacol 1982 21 301-314. 

Vilaro MT, Cortes R, Mengod G. Serotonin 5-HT4 receptors and their mRNAs in rat and guinea pig brain distribution and effects of neurotoxic lesions. J Comp Neurol 2005 484 418-439. 

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