entheogenic-gnosis
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Synthesis and pharmocological profile of a series of 2,5-substituted-N,N-dimethyltryptamine derivitives as novel antagonists for the vascular 5HT1b-like receptor
Authors listed are: Gerard p. Molony, graeme r. Margin, Neil Mathews, heather Hobbs, Susan dodsworth, etc...
Synthesis and pharmacological profile of a series of 2,5-substituted-N,N-dimethyltryptamine derivatives as novel antagonists for the vascular 5-HT1B-like receptor
Unfortunately I have not been able to access the full article, I can only read the abstract, if anyone knows where I would be able to locate the full paper it would be very much appreciated, thank you.
-EG
ABSTRACT:
The coronary 5-HT 1B -like receptor has been implicated in vasospasm and it is postulated that a 5-HT 1B -like antagonist may block the detrimental action of 5-HT whilst not interfering with normal blood vessel function. The synthesis and pharmacological profile of a novel series of 2-(N-heteroaryl)carboxamido-5-substituted-N,N-dimethyltryptamine derivatives as silent (as judged by the inability of angiotensin II to unmask 5-HT 1B -like receptor mediated agonist activity in the rabbit femoral artery), competitive and selective 5-HT 1B -like receptor antagonists is described. Modifications to the 2-carboxamido sidechain as well as the 5-ethylene linked heterocycle are explored. N-Furfuryl-5-[2-(N-phthalimido)ethyl]-3-[2-(dimethylamino)ethyl]-1H-indole-2-carboxamide (34) was discovered which fulfilled our in vitro selection criteria and which had a favourable pharmacokinetic profile. Compound 34 showed good affinity (pK B = 7.38 ) for the vascular 5-HT 1B -like receptor and greater than 125 fold selectivity over α 1 -adrenoceptor affinity. The selectivity of 34 and related compounds for the 5-HT 1B -like receptor over other receptor subtypes is discussed and a mode of binding for this class of compound to a pharmacophore model is proposed.
Authors listed are: Gerard p. Molony, graeme r. Margin, Neil Mathews, heather Hobbs, Susan dodsworth, etc...
Synthesis and pharmacological profile of a series of 2,5-substituted-N,N-dimethyltryptamine derivatives as novel antagonists for the vascular 5-HT1B-like receptor
Unfortunately I have not been able to access the full article, I can only read the abstract, if anyone knows where I would be able to locate the full paper it would be very much appreciated, thank you.
-EG
ABSTRACT:
The coronary 5-HT 1B -like receptor has been implicated in vasospasm and it is postulated that a 5-HT 1B -like antagonist may block the detrimental action of 5-HT whilst not interfering with normal blood vessel function. The synthesis and pharmacological profile of a novel series of 2-(N-heteroaryl)carboxamido-5-substituted-N,N-dimethyltryptamine derivatives as silent (as judged by the inability of angiotensin II to unmask 5-HT 1B -like receptor mediated agonist activity in the rabbit femoral artery), competitive and selective 5-HT 1B -like receptor antagonists is described. Modifications to the 2-carboxamido sidechain as well as the 5-ethylene linked heterocycle are explored. N-Furfuryl-5-[2-(N-phthalimido)ethyl]-3-[2-(dimethylamino)ethyl]-1H-indole-2-carboxamide (34) was discovered which fulfilled our in vitro selection criteria and which had a favourable pharmacokinetic profile. Compound 34 showed good affinity (pK B = 7.38 ) for the vascular 5-HT 1B -like receptor and greater than 125 fold selectivity over α 1 -adrenoceptor affinity. The selectivity of 34 and related compounds for the 5-HT 1B -like receptor over other receptor subtypes is discussed and a mode of binding for this class of compound to a pharmacophore model is proposed.
thank you!