Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UNIPROT:P08908 (5-HT1A)
 5,574 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The role of serotonin (5-HT) in blood pressure (BP) regulation was reviewed. Central and peripheral 5-HT receptors can be divided into three receptor subtypes: 5-HT1 (5-HT1A, 5-HT1B, 5-HT1C), 5-HT2 and 5-HT3 receptors. The selective agonists and antagonists of these receptor subtypes are useful for investigating the BP regulation by 5-HT. The central 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT) produced hypotension and decreases in sympathetic nerve activity (SNA). This suggests that central 5-HT may cause decreases in both BP and SNA via 5-HT1A receptors. Since the 5-HT2 receptor antagonist ketanserin, which has an antihypertensive effect, decreased SNA and the 5-HT2 agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) increased SNA, central 5-HT2 receptors may be connected with the 5-HT-induced increases in both BP and SNA. On the other hand, ketanserin's antihypertensive effects via its 5-HT2 receptor blocking action in the vascular system indicates that peripheral 5-HT may contribute to the initiation or the maintenance of elevated vascular resistance in several forms of hypertension including essential hypertension. However, ketanserin also possesses alpha 1-adrenoceptor blocking action, and its precise antihypertensive mechanism has not been established. Further study of the antihypertensive mechanism of ketanserin will help clarify the precise role of 5-HT in BP regulation.
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PMID:[Serotonin and blood pressure regulation--antihypertensive mechanism of ketanserin]. 257 64

The renal vasodilatating properties of tertatolol demonstrated in animals have been confirmed in man. In a first study [Paillard et al., 1986], tertatolol (T) 5 mg and propranolol (Pr) 160 mg (SR) were given orally for 15 days to 2 groups of 9 patients with essential hypertension. Glomerular filtration rate (GFR), measured by inulin clearance and renal plasma flow (RPF) measured by PAH clearance increased in T group (+8.9%, p = 0.038 and + 13.0%, p = 0.007, respectively) and decreased in Pr group (-2.8%, NS and -13.4%, p < 0.001, respectively). Two clinical pharmacology studies [Leeman et al., 1986; Nitenberg et al., 1990] have shown specific and selective effects of tertatolol on the renal vasculature. In 8 hypertensive patients with chronic renal failure, the effects of tertatolol 5 mg were evaluated before and after 3 months of treatment on GFR using inulin clearance, and RPF, using PAH clearance [Hannedouche et al., 1991]. After 3 months of treatment, GFR and effective RPF increased significantly by 10 and 13%, respectively, whereas RVR decreased by 16% and the filtration fraction was unchanged. In summary, tertatolol 5 mg, contrasting with other beta-blockers, possesses a selective effect on the renal circulation beneficial to hypertensive patients. The mechanisms of this renal vasodilatation are not fully understood but might involve renal 5-HT1A receptor stimulation.
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PMID:Overview of novel renal properties of tertatolol. 790 18

The 5-HT1A receptor is a pharmacologically well characterized serotonin receptor subtype and it has long been investigated because of its involvement in several physiopathological mechanisms and treatment of neurological diseases like ansia and depression. Serotonin (5-HT) also shows many non-neural functions such as essential hypertension, embryogenesis, follicle maturation and behavior. Moreover, it exerts a growth factor function on different types of non-tumoral cells, and it was also found to be related to oncogenes. In fact, growth-stimulatory activity of serotonin in different human tumor cells has been reported. Recently, new chemical molecules binding the 5-HT1A receptor have been described as novel therapeutic entities useful in neuroprotection, cognitive impairment, Parkinson's Disease, pain treatment, malignant carcinoid syndrome and cancer. It was widely demonstrated that 5-HT1A receptor is involved in the carcinogenesis and consequently in many human tumor types, such as prostate, bladder, small cell lung, colonrectal and cholangiocarcinoma. Furthermore, depending on the tumor type, 5-HT1A receptor antagonists were shown to be capable of blocking the 5HT-induced increase in tumor growth. In this review, we have focused our attention on each tumor type where the 5-HT1A receptor is involved, investigating the role of this molecular target and the different classes of compounds that have shown the capability to modulate it. The analyzed aspects could represent a hint for the medical chemists to develop novel molecules as selective 5-HT1A agents are useful in further elucidating the role of this therapeutic target.
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PMID:The Role of 5-HT1A Receptor in Cancer as a New Opportunity in Medicinal Chemistry. 2942 2