Substituted Lysergamide
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Substituted Lysergamide
Lysergamides, also known as ergoamides or as lysergic acid amides, are amides of lysergic acid (LA). They are ergolines, with some lysergamides being found naturally in ergot as well as other fungi. Lysergamides are notable in containing embedded phenethylamine and tryptamine moieties within their ergoline ring system. The simplest lysergamides are ergine (lysergic acid amide; LSA) and isoergine (iso-lysergic acid amide; iso-LSA). In terms of pharmacology, the lysergamides include numerous serotonin and dopamine receptor agonists, most notably the psychedelic drug lysergic acid diethylamide (LSD) but also a number of pharmaceutical drugs like ergometrine, methylergometrine, methysergide, and cabergoline. Various analogues of LSD, such as the psychedelics ALD-52 (1A-LSD), ETH-LAD, LSZ, and 1P-LSD and the non-hallucinogenic 2-bromo-LSD (BOL-148), have also been developed. Ergopeptines like ergotamine, dihydroergotamine, and bromocriptine are also lysergamides, but with a ...
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Lysergamides
Lysergamides, also known as ergoamides or as lysergic acid amides, are amides of lysergic acid (LA). They are ergolines, with some lysergamides being found natural product, naturally in ergot as well as other fungi. Lysergamides are notable in containing embedded substituted phenethylamine, phenethylamine and substituted tryptamine, tryptamine moiety (chemistry), moieties within their ergoline ring system (chemistry), ring system. The simplest lysergamides are ergine (lysergic acid amide; LSA) and isoergine (iso-lysergic acid amide; iso-LSA). In terms of pharmacology, the lysergamides include numerous serotonin and dopamine receptor (biochemistry), receptor agonists, most notably the psychedelic drug lysergic acid diethylamide (LSD) but also a number of pharmaceutical drugs like ergometrine, methylergometrine, methysergide, and cabergoline. Various analogues of LSD, such as the psychedelics ALD-52 (1A-LSD), ETH-LAD, LSZ, and 1P-LSD and the non-hallucinogenic 2-bromo-LSD (BOL-148) ...
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Agonist
An agonist is a chemical that activates a Receptor (biochemistry), receptor to produce a biological response. Receptors are Cell (biology), cellular proteins whose activation causes the cell to modify what it is currently doing. In contrast, an Receptor antagonist, antagonist blocks the action of the agonist, while an inverse agonist causes an action opposite to that of the agonist. Etymology The word originates from the Ancient Greek, Greek word (''agōnistēs''), "contestant; champion; rival" < (''agōn''), "contest, combat; exertion, struggle" < (''agō''), "I lead, lead towards, conduct; drive."


Types of agonists

Receptor (biochemistry), Receptors can be activated by either endogenous agonists (such as hormones and neurotransmitters) or exogenous agonists (such as medication, drugs), resulting in a biological response. A physiological agonism an ...
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Ergotamine
Ergotamine, sold under the brand name Ergomar among others, is an ergopeptine and part of the ergot family of alkaloids; it is structurally and biochemically closely related to ergoline. It is structurally similar to several neurotransmitters, and it acts as a vasoconstrictor. It is used for acute migraines, sometimes with caffeine as the combination ergotamine/caffeine. The drug is a non-selective modulator or agonist of serotonin receptors and other receptors. It is peripherally selective and crosses into the brain in minimal amounts. Medicinal use of ergot fungus began in the 16th century, for the induction of childbirth; but dosage uncertainty discouraged its use. It has been used to prevent post-partum hemorrhage (bleeding after childbirth). It was first isolated from the ergot fungus by Arthur Stoll, at Sandoz in 1918, and was marketed as Gynergen in 1921. Medical uses Ergotamine is indicated as therapy to abort or prevent vascular headache. Available ...
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Ergopeptine
Ergoline is a core structure in many alkaloids and their synthetic derivatives. Ergoline alkaloids were first characterized in ergot. Some of these are implicated in the condition of ergotism, which can take a convulsive form or a gangrenous form. Even so, many ergoline alkaloids have been found to be clinically useful. Annual world production of ergot alkaloids has been estimated at 5,000–8,000 kg of all ergopeptines and 10,000–15,000 kg of lysergic acid, used primarily in the manufacture of semi-synthetic derivatives. Others, such as lysergic acid diethylamide, better known as LSD, a semi-synthetic derivative, and ergine, a natural derivative found in '' Argyreia nervosa'', ''Ipomoea tricolor'' and related species, are known psychedelic substances. Natural occurrence Ergoline alkaloids are found in fungi such as Claviceps purpurea, Claviceps paspali, and the related Periglandula, which have a permanent, symbiotic bond with numerous flowering vines, most notably ...
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1P-LSD
1P-LSD, also known as 1-propanoyl-lysergic acid diethylamide (1-propionyl-LSD), is a psychedelic drug of the lysergamide class that is a derivative and functional analogue of LSD and a homologue of ALD-52. It originated in 2015 when it appeared a designer drug sold online. It was first synthesized as a legal-LSD alternative by Lizard Labs, a Netherlands based research chemical laboratory. It modifies the LSD molecule by adding a propionyl group to the nitrogen atom of LSD's indole group. Pharmacology Like ALD-52, 1P-LSD is believed to act as a prodrug for LSD via hydrolysis of the propionyl group. When 1P-LSD is incubated in human serum, administered intravenously to rats, or administered either orally or intravenously to human subjects, high levels of LSD and relatively low levels of 1P-LSD are quickly detected, demonstrating that 1P-LSD is rapidly hydrolyzed into LSD ''in vivo'' following ingestion. Indeed, following intravenous administration in humans 1P-LSD is detectable ...
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ETH-LAD
ETH-LAD, or ETHLAD, also known as 6-ethyl-6-nor-lysergic acid diethylamide (6-ethyl-6-nor-LSD), is a psychedelic drug of the lysergamide family related to lysergic acid diethylamide (LSD; also known as METH-LAD). It is slightly more potent than LSD and is among the most potent psychedelics known. The drug has been encountered as a novel designer drug in Europe. In addition, a prodrug of ETH-LAD, 1P-ETH-LAD, has been developed and encountered. Use and effects ETH-LAD is slightly more potent than LSD in both animals and humans. It is about 1.6- to 2.3-fold more potent than LSD in rodent drug discrimination tests. The drug's human dose range is 20 to 150μg orally, compared to a range of 50 to 200μg given for LSD, and it is said to be roughly twice as potent as LSD in humans. As such, ETH-LAD is one of the most potent serotonergic psychedelics in humans known, if not the most potent known psychedelic. Moreover, it has been said that LSD can no longer be considered the most pot ...
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ALD-52
ALD-52, also known as 1-acetyl-LSD (1A-LSD), is a psychedelic drug of the lysergamide family related to lysergic acid diethylamide (LSD). It has been reported to produce similar psychoactive effects as LSD, but its pharmacological effects on humans are poorly understood. The drug is assumed to act as a prodrug to LSD in humans, and this has been substantiated ''in vitro''. ALD-52 was initially synthesized in 1957 by Albert Hofmann. The purported first confirmed detection of the substance on the illicit market occurred in April 2016. Use and effects In Entry 26 of his compendium '' TiHKAL'', which discussed LSD, chemist Alexander Shulgin touched briefly on the subject of ALD-52. His comments there are vague, second-hand accounts saying doses in the 50–175 μg range have resulted in various conclusions. One account found that there was less visual distortion than with LSD and it seemed to produce less anxiety and tenseness and that it was somewhat less potent. One subj ...
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Cabergoline
Cabergoline, sold under the brand name Dostinex among others, is a dopaminergic medication used in the treatment of high prolactin levels, prolactinomas, Parkinson's disease, and for other indications. It is taken by mouth. Cabergoline is an ergot derivative and a potent dopamine D2 receptor agonist. Cabergoline was patented in 1980 and approved for medical use in 1993. It is on the World Health Organization's List of Essential Medicines. Medical uses * Lactation suppression * HyperprolactinemiaUK electronic Medicines CompendiuDostinex TabletsLast Updated on eMC Dec 23, 2013 * Adjunctive therapy of prolactin-producing pituitary gland tumors (prolactinomas); * Monotherapy of Parkinson's disease in the early phase; * Combination therapy, together with levodopa and a decarboxylase inhibitor such as carbidopa, in progressive-phase Parkinson's disease; * In some countries also: ablactation and dysfunctions associated with hyperprolactinemia (amenorrhea, oligomenorrhea, anovu ...
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Methysergide
Methysergide, sold under the brand names Deseril and Sansert, is a monoaminergic medication of the ergoline and lysergamide groups which is used in the prophylaxis and treatment of migraine and cluster headaches. It has been withdrawn from the market in the United States and Canada due to safety concerns. It is taken by mouth. The drug is a prodrug of methylergometrine (methylergonovine), which circulates at levels about 10times higher than those of methysergide during treatment with methysergide. Whereas methysergide is a mixed agonist of some serotonin receptors (e.g., the 5-HT1 receptors) and antagonist of other serotonin receptors (e.g., the 5-HT2 receptors), methylergonovine is a non-selective agonist of most of the serotonin receptors, including of both the serotonin 5-HT1 and 5-HT2 receptor subgroups. Methysergide and methylergometrine are ergolines and lysergamides and are related to the ergot alkaloids. Previously thought to be an exclusively synthetic compound, ...
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Methylergometrine
Methylergometrine, also known as methylergonovine and sold under the brand name Methergine, is a medication of the ergoline and lysergamide groups which is used as an oxytocic in obstetrics and as an antimigraine agent in the treatment of migraine headaches. It reportedly produces psychedelic effects similar to those of lysergic acid diethylamide (LSD) at high doses. Previously thought to be an exclusively synthetic compound, it has been reported to occur naturally in '' Argyreia nervosa'' (Hawaiian baby woodrose). The drug is on the World Health Organization's List of Essential Medicines. Medical uses Obstetric use Methylergometrine is a smooth muscle constrictor that mostly acts on the uterus. It is most commonly used to prevent or control excessive bleeding following childbirth and spontaneous or elective abortion, and also to aid in expulsion of retained products of conception after a missed abortion (miscarriage in which all or part of the fetus remains in the uterus) ...
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Ergometrine
Ergonovine, also known as ergometrine and lysergic acid propanolamide, is a medication used to cause contractions of the uterus to treat heavy vaginal bleeding after childbirth. It can be used either by mouth, by injection into a muscle, or injection into a vein. Common side effects include high blood pressure, vomiting, seizures, headache, and low blood pressure. Other serious side effects include ergotism. Ergonovine was discovered in 1932. It is on the World Health Organization's List of Essential Medicines. Ergonovine is controlled in some countries because it can be used to make the psychedelic drug lysergic acid diethylamide (LSD). It is also known to produce psychedelic effects itself at high doses. Medical uses Ergonovine has a medical use in obstetrics to facilitate delivery of the placenta and to prevent bleeding after childbirth by causing smooth muscle tissue in the blood vessel walls to narrow, thereby reducing blood flow. It is usually combined with oxyto ...
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