Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs.
We describe a new class of drugs that selectively block serotonin M-receptors on peripheral neurones. Because of their high affinity, some of these drugs are the most potent of any pharmacological class yet reported. They have allowed the identification of three M-receptor subtypes, one of which is responsible for mediating the painful effects of serotonin in humans.
D000818:Animals; D001920:Bradykinin / Q000494:pharmacology; D002540:Cerebral Cortex; D005260:Female; D006168:Guinea Pigs; D006321:Heart / Q000294:innervation; D006801:Humans; D007082:Ileum; D007211:Indoles / Q000378:metabolism / Q000494:pharmacology; D008297:Male; D009130:Muscle, Smooth / Q000294:innervation; D009474:Neurons / Q000378:metabolism*; D010146:Pain / Q000139:chemically induced; D010525:Peripheral Nerves / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism / Q000502:physiology*; D012701:Serotonin / Q000031:analogs & derivatives / Q000378:metabolism / Q000494:pharmacology; D000077526:Tropisetron; D014630:Vagus Nerve
D007211:Indoles; D011985:Receptors, Serotonin; C042390:alpha-methylserotonin; D012701:Serotonin; D000077526:Tropisetron; C045918:2-methyl-5-HT; D001920:Bradykinin