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The serotonin 5-HT1D receptor: A progress review

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Abstract

Most of the known neurotransmitters interact with more than one type of receptor. Some of them even dispose of receptor subtypes to exert their actions. Serotonin, far from being an exception to that, possesses at least 3 classes of receptors, which have all been reported to be heterogeneous, although convincing data only exist for the 5-HT1 class. This name has been proposed in 1979, two years before the introduction of ‘A’ and ‘B’ in the nomenclature to account for the observed heterogeneity of these cites. The 5-HT1C receptor subtype was first described in 1984 and the last member of the family, named 5-HT1D, was characterized in 1987. The pharmacological profiles, the signal transducing systems and the anatomical localizations, both at the regional and cellular levels, of all these subtypes have been investigated and possible functions have been proposed for each of them. Moreover, last and most definitive demonstration of the subtype individuality, the gene or complementary DNA coding for the 5-HT1A and 5-HT1C (and 5-HT2) receptors have been cloned and sequenced. Such data are still missing for 5-HT1D (and 5-HT1B) receptors, but will certainly be provided in the next few years. However and waiting for this decisive clue, the characterization of the 5-HT1D subtype leaves no doubt concerning its significance as a functional 5-HT receptor. This review will concentrate on the characteristics of this subtype of 5-HT receptor.

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Abbreviations

5-CT:

5-carboxamidotryptamine

5-MeOT:

5-methoxy-tryptamine

5-MeODMT:

N,N-dimethyl-5-methoxytryptamine

8-OH-DPAT:

8-hydroxy-2[di-n-propylamino]tetralin

CYP:

cyanopindolol

DHE:

dihydroergotamine

DOI:

2,5-dimethoxy-4-iodophenylisopropylamine

DP-5-CT:

N,N-dipropyl 5-carboxamidotryptamine

ICPY:

2-iodo-cyanopindolol

mCPP:

m-chloro-phenyl-piperazine

TFMPP:

m-trifluoro-methyl-phenyl-piperazine

EMAX :

Maximal effect

EC50 :

Half maximal effective concentration

KD :

Dissociation constant

KB :

Antagonist dissociation constant

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    Christian Waeber, Philippe Schoeffter, Daniel Hoyer & José M. Palacios

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Waeber, C., Schoeffter, P., Hoyer, D. et al. The serotonin 5-HT1D receptor: A progress review. Neurochem Res 15, 567–582 (1990). https://doi.org/10.1007/BF00973745

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