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Journal of Experimental Biology 56,311-321 (1972)
Published by Company of Biologists 1972

The Mode of Action Of 5-Hydroxytryptamine

M. J. BERRIDGE 1

1 A.R.C. Unit of Invertebrate Chemistry and Physiology, Department of Zoology, Downing Street, Cambridge

1. The isolated salivary gland of the blowfly Calliphora has been used to study the molecular pharmacology of 5-hydroxytryptamine (5-HT).

2. Ethylamine alone is inactive but the addition of extra carbon atoms or ring systems (imidazole or benzene) introduces some activity. A 5-hydroxyindole ring confers most activity.

3. If the hydroxyl group is either removed, replaced with other groups, or displaced to the 4- or 6-position on the indole ring there is a large reduction in activity.

4. The activity of the molecule is greatly reduced if the length of the side chain is decreased (gramine) or increased (3-aminopropyl indole) by a single carbon atom. Such molecules are effective competitors.

5. These structure-activity studies suggest that the specificity of 5-HT resides in the 5-hydroxyindole moiety which binds the molecule to the receptor while the positively charged ethylamine side chain is responsible for inducing the hormonal effect.

Submitted on July 29, 1971


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W. Chernick, E. Bobyock, and P. Bradford
5-Hydroxytryptamine Modulation of Rat Parotid Salivary Gland Secretion
Journal of Dental Research, January 1, 1989; 68(1): 59 - 63.
[Abstract] [PDF]


© The Company of Biologists Ltd 1972