Spezifische Hemmung von 5-Oxytryptamin-Effekten durch Lysergs�uredi�thylamid und �hnliche K�rper

QSAR studies on hallucinogens

“…59 For the data given in Table VII, the correlation equations obtained were n = 17, r = 0.926, s = 0.23, P2>14 = 42.05 (22) was assigned a value of 0 for compounds With the exclusion of compounds 73 and 74, which were much less active than predicted from their log P values, Nichols et al35 were however able to correlate this agonistic activity of phenylalkylamines with quite high degree of significance with log P alone, but the equation obtained was of third order (eq 23). In eq log RBR = 0.23 -0.89 log P + 0.95(log P)2 -0.16(log P)3 In the PPP-SCF results, however, were included only ZV,7V-dimethyltryptamine (DMT, 81) analogues [81][82][83][84][85][86][87][88][89] and in the CNDO/2 results only methoxy derivatives of DMT (81-86) were included. Besides, 86 was not included in deriving eq 28 and 33.…”

The LSD-Psychosis: I. Pharmacological Aspects of the LSD Psychosis.

“…Serotonin has the ability to potentiate the barbiturate narcosis in various laboratory animals. It has been shown many times that this potentiating effect can be inhibited by LSD in mice (11,35,46,47,50), as well as in rats (7) and rabbits (8), but this antagonism does not appear to be related to the hallucinogenic property of the drug, since the same antagonism can be demonstrated with the nonhallucinogenic substance BOL-148 (50). If introduced into a cerebral ventricle, 5-HT produces a lethargic state in the cat, a cataleptic condition in the dog.…”

“…It is, however, not very likely that this peripheral serotonin antagonism has anything to do with the hallucinogenic property of the drug. The brom-derivative BOL-148 has no hallucinogenic effect, in spite of its anti-5-HT potency being of the same magnitude as that of LSD (11,12,31). The acetyl and methyl derivatives of LSD (compounds ALD-52 and MLD-41) show a significantly higher antiserotonin activity than LSD (10) but are less hallucinogenic.…”

Serotonin in Relation to Brain Function: I. The Pharmacology of Serotonin (5-HT) (A Survey).

“…On the rabbit ear, LSD is more effective than bromo-LSD in blocking 5-HT vasoconstriction (83), but unlike bromo-LSD, LSD itself induces vasoconstriction in high doses. Bromo-LSD is a more potent blocking agent than LSD on rat estrous uterus (16,93). On guinea pig ileum and rabbit intestine, bromo-LSD effectively antagonizes 5-HT, without itself stimulating; LSD stimulates these preparations and fails to show 5-HT antagonism (93).…”

“…Several groups have studied the effects of 5-HT on "spontaneous activity" in mice and rats and on the so-called potentiation of barbiturate hypnosis (i.e., prolongation of sleeping time) (13,15,16,82,88). 5-HT depresses spontaneous activity as does bromo-LSD, while LSD stimulates.…”