Protein Information

Name 5 HT1D
Synonyms 5 HT 1D; 5 HT 1D alpha; 5 HT1D; 5 hydroxytryptamine (serotonin) receptor 1D; 5 hydroxytryptamine 1D receptor; HT1DA; HTR1D; HTR1DA…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
11216445 Villalon CM, Centurion D, Sanchez-Lopez A, De Vries P, Saxena P: 5-HT receptors mediating external carotid vasoconstriction in vagosympathectomized dogs. Zhongguo Yao Li Xue Bao. 1999 Dec;20(12):1057-67.

With the advent of subtype-selective antagonists it was subsequently shown that external carotid vasoconstriction to 5-HT and sumatriptan is dose-dependently antagonized by the selective 5-HT1B receptor antagonist SB224289 (2,3,6,7-tetrahydro-1'-methyl-5-[2'-methyl-4' (5-methyl-1,2,4-oxadiazol-3-yl) biphenyl-4-carbonyl] furo [2,3-f] indole-3-spiro-4'-piperidine hydrochloride), whereas the selective 5-HT1D receptor antagonist BRL15572 (1-(3-chlorophenyl)-4-[3,3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride) was ineffective.
32(0,1,1,2) Details
14744615 Villalon CM, Centurion D, Willems EW, Arulmani U, Saxena PR, Valdivia LF: 5-HT1B receptors and alpha 2A/2C-adrenoceptors mediate external carotid vasoconstriction to dihydroergotamine. Eur J Pharmacol. 2004 Jan 26;484(2-3):287-90.

This response was: (1) partly blocked in dogs pretreated intravenously with the antagonists SB224289 (5-HT (1B); 2,3,6,7-tetrahydro-1'-methyl-5-[2'-methyl-4' (5-methyl-1,2,4-oxadiazol-3-yl) biphenyl-4-carbonyl] furo [2,3-f] indole-3-spi ro-4'-piperidine hydrochloride), rauwolscine (alpha (2)), BRL44408 (alpha (2A); 2-[2H-(1-methyl-1,3-dihydroisoindole) methyl]-4,5-dihydroimidazole) or MK912 (alpha (2C); (2S,12bS)-1'3'-dimethylspiro (1,3,4,5',6,6',7,12b-octahydro-2Hbenzo [b] furo [ 2,3-a] quinazoline)-2,4'-pyrimidin-2'-one); (2) markedly blocked after SB224289 plus rauwolscine; and (3) unaffected after BRL15572 (5-HT (1D); 1-(3-chlorophenyl)-4-[3,3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride) or imiloxan (alpha (2B)).
31(0,1,1,1) Details
16173953 Calama E, Ortiz de Urbina AV, Moran A, Martin ML, San Roman L: Effect of 5-hydroxytryptamine on neurogenic vasoconstriction in the isolated, autoperfused hindquarters of the rat. Clin Exp Pharmacol Physiol. 2005 Oct;32(10):894-900.

The effects of 5-HT were mimicked by 5-carboxamidotryptamine (a 5-HT1 receptor agonist) and L-694 247 (a selective 5-HT1D receptor agonist), but not by 8-hydroxy-2-dipropylaminotetralin (a 5-HT1A receptor agonist), CGS-12066B (a 5-HT1B receptor agonist), alpha-methyl-5-HT (a 5-HT2 receptor agonist), 1-(3-chlorophenyl) piperazine (a 5-HT2C receptor agonist) or 1-phenylbiguanide (a 5-HT3 receptor agonist).
The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibited the effect of the agonist L-694 247. 4.
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17584957 Papageorgiou A, Denef C: Stimulation of growth hormone release by 5-hydroxytryptamine (5-HT) in cultured rat anterior pituitary cell aggregates: evidence for mediation by 5-HT2B, 5-HT7, 5-HT1B, and ketanserin-sensitive receptors. Endocrinology. 2007 Sep;148(9):4509-22. Epub 2007 Jun 21.

The present data suggest that 5-HT may release GH through a pituitary site of action, and that the 5-HTR2B, 5-HTR7 and 5-HTR1B mediate this response, with possibly an inhibitory component of the 5-HTR1D.
Basal GH release was stimulated by the 5-HTR2 agonists 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane, m-chlorophenyl piperazine, and alpha-methyl 5-HT; 5-carboxytryptamine (agonist at 5-HTR1, -5, and -7); tryptamine (preferential 5-HTR7 agonist); and the selective 5-HTR1B agonist CP93129 but not the 5-HTR1A agonists 7-(dipropylamino) tetralin-1-ol-8-hydroxy-2-(di-n-propylamino) tetralin and the 5-HTR1B/D agonist sumatriptan.
1(0,0,0,1) Details
11888550 Millan MJ, Newman-Tancredi A, Lochon S, Touzard M, Aubry S, Audinot V: Specific labelling of serotonin 5-HT (1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H] GR125,743. Pharmacol Biochem Behav. 2002 Apr;71(4):589-98.

These rank orders of affinity correspond to the binding profile of 5-HT (1B) rather than 5-HT (1D) receptors.
In competition binding studies, affinities were determined for 15 chemically diverse 5-HT (1B) agonists, including 2-[5-[3-(4-methylsulphonylamino) benzyl-1,2,4-oxadiazol-5-yl]-1H-indole-3-y l] ethylamine (L694,247; pK (i), 10.4), 5-carboxamidotryptamine (5-CT; 9.7), 3-[3-(2-dimethylamino-ethyl)-1H-indol-6-yl]-N-(4-methoxybenzyl) acrylamide (GR46,611; 9.6), 5-methoxy-3-(1,2,5,6-tetrahydro-4-pyridinyl)-1H-indole (RU24,969; 9.5), dihydroergotamine (DHE; 8.6), 5-H-pyrrolo [3,2-b] pyridin-5-one,1,4-dihydro-3-(1,2,3,6-tetrahydro-4-pyridi nyl (CP93,129; 8.4), anpirtoline (7.9), sumatriptan (7.4), 1-[2-(3-fluorophenyl) ethyl]-4-[3-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl] pro pyl] piperazine (L775,606; 6.4) and (minus sign)-1 (S)-[2-[4-(4-methoxyphenyl) piperazin-1-yl] ethyl]-N-methyl-3,4-dihyd ro-1H-2-benzopyran-6-carboxamide (PNU109,291; <5.0).
1(0,0,0,1) Details
15452415 Calama E, Moran A, Ortiz de Urbina AV, Martin ML, San Roman L: m-CPP, a 5-HT2C receptor agonist that modifies the perfusion pressure of the hindquarter vascular bed of anesthetized rat. Pharmacology. 2005 Feb;73(2):70-5. Epub 2004 Sep 27.

Both vasodilatation and vasoconstriction were inhibited by the 5-HT (1,2 ) receptor antagonist methiothepin, whereas the 5-HT (2 ) receptor antagonist ritanserin blocked only the vasoconstrictor responses. 1-[4-(1-Adamantanecarboxamido) butyl]-4-(2-methoxyphenyl) piperazine (a 5-HT (1A) receptor antagonist) and ICI 118,551 (a beta (2)-receptor antagonist) failed to modify the vasodilator responses of m-CPP.
Both BRL 15572 (a 5-HT (1D) receptor antagonist) and GR 55562 (a 5-HT (1B) receptor antagonist) only partially inhibited this action.
1(0,0,0,1) Details
15866558 Tsaltas E, Kontis D, Chrysikakou S, Giannou H, Biba A, Pallidi S, Christodoulou A, Maillis A, Rabavilas A: Reinforced spatial alternation as an animal model of obsessive-compulsive disorder (OCD): investigation of 5-HT2C and 5-HT1D receptor involvement in OCD pathophysiology. Biol Psychiatry. 2005 May 15;57(10):1176-85.

1(0,0,0,1) Details
11070185 Shaw AM, Bunton DC, Brown T, Irvine J, MacDonald A: Regulation of sensitivity to 5-hydroxytryptamine in pulmonary supernumerary but not conventional arteries by a 5-HT (1D)-like receptor. Eur J Pharmacol. 2000 Nov 10;408(1):69-82.


Neither the selective 5-HT (1D) receptor antagonist (1-(3-chlorophenyl)-4-[3, 3-diphenyl (2-(S,R) hydroxypropanyl) piperazine] hydrochloride (BRL15572) nor the 5-HT (1B) receptor antagonist (2,3,6, 7-tetrahydro-1'-methyl-5-[2'methyl-4'5-(methyl-1,2,4-oxadiazol-3-y l) biphenyl-4-carbonyl] furo [2,3-f] indole-3-spiro-4'-piperidine hydrochloride (SB224289) antagonised concentration-response curves induced by 5-HT or 5-HT (1)-receptor-selective agonists.
0(0,0,0,0) Details
16153839 Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, Hadley MS, Price GW, Scott CM, Dawson LA: Identification of a potent and selective 5-HT1B receptor antagonist. . Bioorg Med Chem Lett. 2005 Nov 1;15(21):4708-12.

An SAR study around the mixed 5-HT1ABD receptor antagonist SB-272183 found that introduction of cis-2,6-dimethyl substitution onto the piperazine ring was a key structural change, which imparted a combination of both excellent selectivity over the 5-HT1A and 5-HT1D receptors and low intrinsic activity.
31(0,1,1,1) Details
11350497 Fernandez MM, Calama E, Moran A, Martin ML, San Roman L: Characterization of mechanisms involved in presynaptic inhibition of sympathetic pressor effects induced by some 5-HT1 receptor antagonists. J Auton Pharmacol. 2000 Oct-Dec;20(5-6):313-23.


In a previous study, we showed that the presynaptic inhibitory action of 5-hydroxytryptamine receptor agonists on sympathetic pressor effects obtained in the pithed rats were mainly mediated by activation of 5-HT1A and 5-HT1D receptor subtypes.
1(0,0,0,1) Details