Drugs online research references
Biochim Biophys Acta. 1976 Jun 23;437(1):150-7.
Histamine (H2) receptor-adenylate cyclase system in pig skin (epidermis).
Iizuka Hadachi K, Halprin KM, Levine V.
Histamine activated adenylate cyclase in pig skin (epidermal) slices, resulting in the accumulation of cyclic AMP. This effect was highly potentiated by the addition of cyclic AMP-phosphodiesterase inhibitors (theophylline, papaverine). A specific H2 receptor inhibitor (metiamide) inhibited the effect of histamine completely, while other antihistamines (diphenhydramine, acetophenazine, perphenazine, fluphenazine, promethazine) inhibited the effect of histamine to various lesser degrees. It has been shown that both epinephrine and prostaglandin E stimulate epidermal adenylate cyclase. Our data using specific blocking agents indicate that histamine, epinephrine and prostaglandin E2 act independently on the epidermal adenylate cyclase system.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7311&dopt=Abstract
Biol Psychiatry. 1991 Aug 15;30(4):349-56.
Decreased histamine H1 receptors in the frontal cortex of brains from patients with chronic schizophrenia.
Nakai T, Kitamura N, Hashimoto T, Kajimoto Y, Nishino N, Mita T, Tanaka C.
Department of Pharmacology, Kobe University School of Medicine, Japan.
Involvement of histamine H1 receptor in the brains of schizophrenic patients was investigated using 3H-mepyramine as a ligand. The specific 3H-mepyramine binding in the frontal cortex was saturable with the dissociation constant (Kd) of about 0.6 nM and the maximum number of binding sites (Bmax) of 64 fmol/mg protein. Specific H1 antagonists, mepyramine (Ki = 1.4 nM), promethazine (Ki = 1.4 nM), diphenylpyraline (Ki = 4.1 nM), triprolidine (Ki = 5.3 nM), diphenylhydramine (Ki = 35 nM), but not the specific H2 antagonist, cimetidine (Ki greater than 10(5) nM), strongly inhibited the 3H-mepyramine binding. Regional distribution of the specific 3H-mepyramine binding was in the order of: frontal cortex greater than hippocampus greater than cerebellum greater than hypothalamus greater than thalamus, putamen, and pallidum. The specific 3H-mepyramine binding in schizophrenic brains was reduced by 56% in the frontal cortex. Representative Scatchard analyses of the specific 3H-mepyramine binding revealed changes resulting from a decrease in receptor density but not in receptor affinity. Down-regulation of the histamine H1 receptor in the frontal cortex may be involved in the pathophysiology of schizophrenia.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1912125&dopt=Abstract
Jpn J Pharmacol. 1977 Dec;27(6):781-9.
Purification of histamine receptor (VI). An improved double labeling method with "double protection".
Uchida M.
Studies were done on the specific labeling of the histaminergic H1-receptor of the longitudinal smooth muscle of cat small intestine. A procedure involving 'double protection' combined with the double labeling technique was developed. The first protection was the usual with a protective antihistamine, promethazine, and the second was cross protection of non-specific sites with non-hitaminergic drugs, thioriazine and atropine. Muscle tissue protected with promethazine against non-radioactive dibenamine was treated with 3H-dibenamine in the presence of these second protectors. The second protectors covered non-receptor sites which had been protected from non-radioactive dibenamine with promethazine. The dose-response curves were carefully checked in each experiment to confirm that the second protectors did not interfere with the specific coverage provided by the first protector. Finally 14C-dibenamine was applied to measure non-specific binding after which the labeled muscles were fractionated and the radioactivity was counted. The specificity of labeling achieved in the receptor-rich fraction by this method is discussed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=609149&dopt=Abstract
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