Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0020672 (hypothermia)
 17,327 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of 2-phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives was examined for the ability to inhibit both rat brain imipramine receptor binding and the synaptosomal uptake of norepinephrine (NE) and serotonin (5-HT). Neurotransmitter uptake inhibition was highest for a subset of 2-phenyl-2-(1-hydroxycyclohexyl)dimethylethylamines in which the aryl ring has a halogen or methoxy substituent at the 3- and/or 4-positions. Potential antidepressant activity in this subset was assayed in three rodent models--the antagonism of reserpine-induced hypothermia, the antagonism of histamine-induced ACTH release, and the ability to reduce noradrenergic responsiveness in the rat pineal gland. An acute effect seen in the rat pineal gland with several analogues, including 1-[1-(3,4-dichlorophenyl)-2-(dimethylamino)ethyl]cyclohexanol (23) and 1-[2-(dimethylamino)-1)-(4-methoxyphenyl)ethyl]cyclohexanol (4), was taken as a possible correlate of a rapid onset of antidepressant activity. Compound 4 (venlafaxine) is presently undergoing clinical evaluation.
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PMID:2-Phenyl-2-(1-hydroxycycloalkyl)ethylamine derivatives: synthesis and antidepressant activity. 197 13

U-43,465F (8-chloro-1-[2-(dimethylamino)ethyl]-6-phenyl-4H-s-triazolo [4,3-a][1,4]benzodiazepine p-toluene sulfonate) showed two fold activity at 32 mg/kg i.p.: antipunishment activity inhibited by the benzodiazepine receptor antagonist Ro 15-1788, and an antidepressant-like reversal of apomorphine-induced hypothermia, antagonized by the beta-adrenergic receptor blocker d,1-propranolol. U-43,465F hence produced effects not mediated by benzodiazepine receptors and these effects might be related to antidepressant activity.
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PMID:U 43,465F: a benzodiazepine with antidepressant activity? Interaction with Ro 15-1788 and d,1-propranolol. 612 34