geoscience.net logo
+ Resolve Article
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter

+ Translate
+ Subscribe to Site Feed
GeoScience Most Shared ContentMost Shared Content

Allosteric regulation by oleamide of the binding properties of 5-hydroxytryptamine7 receptors


, : Allosteric regulation by oleamide of the binding properties of 5-hydroxytryptamine7 receptors. Biochemical Pharmacology 58(11): 1807-1813, Dec 1

Oleamide belongs to a family of amidated lipids with diverse biological activities, including sleep induction and signaling modulation of several 5-hydroxytryptamine (5-HT) receptor subtypes, including 5-HT1A, 5-HT2A/2C, and 5-HT7. The 5-HT7 receptor, predominantly localized in the hypothalamus, hippocampus, and frontal cortex, stimulates cyclic AMP formation and is thought to be involved in the regulation of sleep-wake cycles. Recently, it was proposed that oleamide acts at an allosteric site on the 5-HT7 receptor to regulate cyclic AMP formation. We have further investigated the interaction between oleamide and 5-HT7 receptors by performing radioligand binding assays with HeLa cells transfected with the 5-HT7 receptor. Methiothepin, clozapine, and 5-HT all displaced specific (3H)5-HT (100 nM) binding, with pKD values of 7.55, 7.85, and 8.39, respectively. Oleamide also displaced (3H)5-HT binding, but the maximum inhibition was only 40% of the binding. Taking allost eric (see below) cooperativity into account, a KD of 2.69 nM was calculated for oleamide. In saturation binding experiments, oleamide caused a 3-fold decrease in the affinity of (3H)5-HT for the 5-HT7 receptor, without affecting the number of binding sites. A Schild analysis showed that the induced shift in affinity of (3H)5-HT reached a plateau, unlike that of a competitive inhibitor, illustrating the allosteric nature of the interaction between oleamide and the 5-HT7 receptor. Oleic acid, the product of oleamide hydrolysis, had a similar effect on (3H)5-HT binding, whereas structural analogs of oleamide, trans-9,10-octadecenamide, cis-8,9-octadecenamide, and erucamide, did not alter (3H)5-HT binding significantly. The findings support the hypothesis that oleamide acts via an allosteric site on the 5-HT7 receptor regulating receptor affinity.

US$19.90

PMID: 10571256

DOI: 10.1016/s0006-2952(99)00274-9


Other references

Martínez-Cordero, E.; León, D.E.A.; Novelo-Retana, V.; Hernández-Pando, R.; Uribe-Uribe, N., 2007: Immunohistochemical demonstration of the causative antigen in pigeon hypersensitivity pneumonitis. Chest 132(4): 457a-1-457a-2

Chen, H.; Chang, C.; Yen, C.; Shen, Y., 1980: A serological survey on porcine parvovirus infection in pigs in Taiwan. Chung hua min kuo shou i hsueh hui tsa chih = Journal of the Chinese Society of Veterinary Science 6(1): 51-52

Rukewe, A.; Afuwape, O.O.; Ugheoke, A.; Fatiregun, A.A., 2016: Single-shot lamina thoracic paravertebral block with ketofol for modified radical mastectomy. NlmCategory="UNASSIGNED">We describe the use of single-shot lamina thoracic paravertebral block (TPVB) with sedation for a 56-year-old female patient who had modified radical mastectomy with axillary clearance. Two years ago, she suff...

Anon., 1957: International Veterinary Meeting. Phnom-Penh (14-15 December 1956). At this meeting the rinderpest situation and plans for its control in Cambodia, Laos, Thailand and Vietnam were discussed. The director of veterinary services of Cambodia reported a decrease in the number of outbreaks in 1956 which he ascribed to...

Helasoja, V.; Prättälä, R.; Klumbiene, J.; Petkeviciene, J.; Kasmel, A.; Lipand, A.; Uutela, A.; Puska, P., 2001: Smoking and passive smoking in Estonia, Lithuania and Finland. Identifying target groups of tobacco policy. The aim of this study was to identify population groups which are the most crucial as targets for anti-tobacco action. A comparison was made of the prevalence and patterns of smoking and passive smoking in Estonia, Finland and Lithuania. Total exp...

Kajo, K.; Macháleková, K.; Kviatkovská, Z., 2006: Mammary carcinoma with osteoclast-like giant cells--report of two cases. Authors describe two cases of a rare type of mammary carcinoma occurring in 47-year and 49-year-old women, characterised by osteoclast-like giant cells, hypervascular stroma, and signs of older and recent haemorrhages on the background of the conv...

Florendo, N.T.; Pitcock, J.A.; Muirhead, E.E., 1978: Cyclic 3 5 nucleotide phospho di esterase cytochemical localization in rat reno medullary interstitial cells phospho di esterase in rat renal medulla. The localization of cyclic[c]3',5'-nucleotide phosphodiesterase activity in rat renal papillae was examined by utilizing cytochemical methods. Renal medullary interstitial cells had predictable phosphodiesterase activity predominantly on...

Cummings, L.A.; Rassoulian Barrett, S.; Fellnerova, I.; Cookson, B.T., 2002: Antigens recognized by T cells in response to Salmonella infection Diversity and regulation. Infection with attenuated Salmonella provides long lasting protection against subsequent challenge with virulent strains for both mice and humans. To better understand the mechanisms by which T cells contribute to immunity, we characterized the di...

Pruszynska-Gondek, M., 1979: Rusts occurring on forage and vegetable leguminous plants in the region of Krakow. Acta agraria et silvestria Series agraria: 8 (2) 67-81

Zindel, L.R.; Kranzler, H.R., 2014: Pharmacotherapy of alcohol use disorders: seventy-five years of progress. Modern pharmacotherapy for alcohol dependence has its roots in the failure of National Prohibition in the United States and the rise of the disease model of alcoholism (embodied in Alcoholics Anonymous). In 1948, disulfiram was the first medicatio...