5-HT1A receptor agonists

Agonists of 5-HT1A receptors are divided into partial (partial) and full agonists .

Content

List of 5-HT1A receptor agonists

Complete 5-HT1A receptor agonists

8-OH-DPAT ^[1]
Alnespiron ^[2] ^[3] ^[4]
Befiradol . ^[5] ^[6] ^[7] ^[8] ^[9] ^[10]
Eptapiron ^[11] ^[12]
F-15,599 ^[13] ^[14]
Lesopitron ^[15]
LY-293,284 ^[16] ^[17]
Osemozotan ^[18]
Repinotan ^[19] ^[20]
U-92,016-A ^[21] ^[22]

Partial agonists of 5-HT1A receptors

Partial agonists are agonists that show less ability to stimulate the receptor than full agonists.

Partial agonists of the 5-HT1A serotonin receptor are many substances and drugs , including a number of antidepressants , non-benzodiazepine anxiolytics , typical and atypical antipsychotics , as well as some hallucinogens and empathogens , some anti-migraine , anti-parkinsonian , hypotensive drugs.

Antidepressants

Trazodon
Nefazodon
Vilazodon
Vortioxetine

Nonbenzodiazepine anxiolytics

Binospiron
Buspirone
Gepiron
Zalospiron
Cannabidiol
Ipsapiron
Perospiron
Tandospiron
Thiospiron

Atypical antipsychotics

Aripiprazole
Asenapine
Ziprasidone
Quetiapine
Clozapine
Lurazidone
Olanzapine

Typical Antipsychotics

Haloperidol

Antihypertensives

Urapidil
Rauwolscin

Anti-migraine drugs

Ergotamine
Dihydroergotamine

Hallucinogens

LSD
Psilocin
Psilocybin

Empathogens

MDMA

Dopaminergic anti-Parkinsonian drugs

Lizurid

Libido and Sexual Drugs

Yohimbine

Miscellaneous and research preparations

5-carboxamidotryptamine (5-CT)
5-methoxytryptamine (5-MT)
5-MeO-DMT
Adatanserin
Flibanserin
Alpha ethyltryptamine (αET)
Alpha Methyltryptamine (αMT)
Bay r 1531
Befiradol
Bufotenin
Eltoprazine
Etoperidone
F-11,461
F-12.826
F-13,714
F-14.679
Flesinoxane
Ginkgo Biloba ^[23]
LY-301,317
Ebalzotan
Naluzotan
Piclozotan
Sarisotan
NBUMP
RU-24,969
S-15,535
SSR-181,507
Sunepitron
Trifluoromethylphenylpiperazine
Xaliproden

Notes

↑ Winsauer PJ, Rodriguez FH, Cha AE, Moerschbaecher JM Full and partial 5-HT1A receptor agonists disrupt learning and performance in rats // J. Pharmacol. Exp. Ther. : journal. - 1999 .-- January ( vol. 288 , no. 1 ). - P. 335—347 . - PMID 9862788 .
↑ Griebel G., Misslin R., Pawlowski M., Guardiola Lemaître B., Guillaumet G., Bizot-Espiard J. Anxiolytic-like effects of a selective 5-HT1A agonist, S20244, and its enantiomers in mice. (English) // Neuroreport. : journal. - 1992. - Vol. 3 , no. 1 . - P. 84-86 . - DOI : 10.1097 / 00001756-199201000-00022 . - PMID 1351756 .
↑ Simon P., Guardiola B., Bizot-Espiard J., Schiavi P., Costentin J. 5-HT1A receptor agonists prevent in rats the yawning and penile erections induced by direct dopamine agonists. (Eng.) // Psychopharmacology : journal. - Springer , 1992. - Vol. 108 , no. 1-2 . - P. 47-50 . - DOI : 10.1007 / BF02245284 . - PMID 1357709 .
↑ Astier B., Lambás Señas L., Soulière F., Schmitt P., Urbain N., Rentero N., Bert L., Denoroy L., Renaud B., Lesourd M., Muñoz C., Chouvet G. In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity. (English) // Eur J Pharmacol. : journal. - 2003. - Vol. 459 , no. 1 . - P. 17-26 . - DOI : 10.1016 / S0014-2999 (02) 02814-5 . - PMID 12505530 .
↑ Bardin L., Tarayre JP, Malfetes N., Koek W., Colpaert FC Profound, non-opioid analgesia produced by the high-efficacy 5-HT (1A) agonist F 13640 in the formalin model of tonic nociceptive pain ) // Pharmacology: journal. - 2003 .-- April ( vol. 67 , no. 4 ). - P. 182-194 . - DOI : 10.1159 / 000068404 . - PMID 12595749 .
↑ Bruins Slot LA, Koek W., Tarayre JP, Colpaert FC Tolerance and inverse tolerance to the hyperalgesic and analgesic actions, respectively, of the novel analgesic, F 13640 (English) // European Journal of Pharmacology : journal. - 2003 .-- April ( vol. 466 , no. 3 ). - P. 271—279 . - DOI : 10.1016 / S0014-2999 (03) 01566-8 . - PMID 12694810 .
↑ Bardin L., Assié MB, Pélissou M., Royer-Urios I., Newman-Tancredi A., Ribet JP, Sautel F., Koek W., Colpaert FC Dual, hyperalgesic, and analgesic effects of the high-efficacy 5 -hydroxytryptamine 1A (5-HT1A) agonist F 13640 [(3-chloro-4-fluoro-phenyl) - [4-fluoro-4 - {[(5-methyl-pyridin-2-ylmethyl) -amino] -methyl} piperidin-1-yl] methanone, fumaric acid salt]: relationship with 5-HT1A receptor occupancy and kinetic parameters (Eng.) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 2005 .-- March ( vol. 312 , no. 3 ). - P. 1034-1042 . - DOI : 10.1124 / jpet.104.077669 . - PMID 15528450 .
↑ Colpaert FC, Deseure K., Stinus L., Adriaensen H. High-efficacy 5-hydroxytryptamine 1A receptor activation counteracts opioid hyperallodynia and affective conditioning (Eng.) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 2006 .-- February ( vol. 316 , no. 2 ). - P. 892-899 . - DOI : 10.1124 / jpet.105.095109 . - PMID 16254131 .
↑ Deseure K., Bréand S., Colpaert FC Curative-like analgesia in a neuropathic pain model: parametric analysis of the dose and the duration of treatment with a high-efficacy 5-HT (1A) receptor agonist (eng.) // European Journal of Pharmacology : journal. - 2007 .-- July ( vol. 568 , no. 1-3 ). - P. 134-141 . - DOI : 10.1016 / j.ejphar.2007.04.0.022 . - PMID 17512927 .
↑ Bernard Vacher, Bernard Bonnaud, Wouter Koek. Pyridin-2-yl-methylamine derivatives, method of preparing and application as medicine. US Patent 6020345, May 21, 1999.
↑ Koek W., Patoiseau JF, Assié MB, et al. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential (English) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 1998 .-- October ( vol. 287 , no. 1 ). - P. 266-283 . - PMID 9765347 .
↑ Prinssen EP, Colpaert FC, Koek W. 5-HT1A receptor activation and anti-cataleptic effects: high-efficacy agonists maximally inhibit haloperidol-induced catalepsy (English) // European Journal of Pharmacology : journal. - 2002. - October ( vol. 453 , no. 2-3 ). - P. 217-221 . - DOI : 10.1016 / S0014-2999 (02) 02430-5 . - PMID 12398907 .
↑ Maurel JL, Autin JM, Funes P., Newman-Tancredi A., Colpaert F., Vacher B. High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity ( Journal ) // Journal of Medicinal Chemistry : journal. - 2007 .-- October ( vol. 50 , no. 20 ). - P. 5024-5033 . - DOI : 10.1021 / jm070714l . - PMID 17803293 .
↑ Newman-Tancredi A., Martel JC, Assié MB, et al. Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist (Eng.) // British Journal of Pharmacology : journal. - 2009 .-- January ( vol. 156 , no. 2 ). - P. 338-353 . - DOI : 10.1111 / j.1476-5381.2008.00001.x . - PMID 19154445 .
↑ Haj-Dahmane S., Jolas T., Laporte AM, et al. Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat // English Journal of Pharmacology : journal. - 1994 .-- April ( vol. 255 , no. 1-3 ). - P. 185-196 . - DOI : 10.1016 / 0014-2999 (94) 90097-3 . - PMID 8026543 .
↑ Monte AP, Marona-Lewicka D., Lewis MM, Mailman RB, Wainscott DB, Nelson DL, Nichols DE Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity (Eng.) // Journal of Medicinal Chemistry : journal. - 1998 .-- June ( vol. 41 , no. 12 ). - P. 2134-2145 . - DOI : 10.1021 / jm980076u . - PMID 9622555 .
↑ Foreman MM, Fuller RW, Rasmussen K., Nelson DL, Calligaro DO, Zhang L., Barrett JE, Booher RN, Paget CJ, Flaugh ME Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity .) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 1994 .-- September ( vol. 270 , no. 3 ). - P. 1270-1281 . - PMID 7523657 .
↑ Matsuda T. , Yoshikawa T. , Suzuki M. , Asano S. , Somboonthum P. , Takuma K. , Nakano Y. , Morita T. , Nakasu Y. , Kim HS Novel benzodioxan derivative, 5- (3 - [( (2S) -1,4-benzodioxan-2-ylmethyl) amino propoxy) -1,3-benzodioxole HCl (MKC-242), with a highly potent and selective agonist activity at rat central serotonin1A receptors.] / / Japanese journal of pharmacology. - 1995. - Vol. 69, no. 4 . - P. 357-366. - PMID 8786639 .
↑ De Vry J. , Schohe-Loop R. , Heine HG , Greuel JM , Mauler F. , Schmidt B. , Sommermeyer H. , Glaser T. Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist . (Eng.) // The Journal of pharmacology and experimental therapeutics. - 1998. - Vol. 284, no. 3 . - P. 1082-1094. - PMID 9495870 .
↑ Dong J. , de Montigny C. , Blier P. Full agonistic properties of BAY x 3702 on presynaptic and postsynaptic 5-HT1A receptors electrophysiological studies in the rat hippocampus and dorsal raphe. (Eng.) // The Journal of pharmacology and experimental therapeutics. - 1998. - Vol. 286, no. 3 . - P. 1239-1247. - PMID 9732384 .
↑ Romero AG, Leiby JA, McCall RB, Piercey MF, Smith MW, Han F. Novel 2-substituted tetrahydro-3H-benz [e] indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants . (Eng.) // J Med Chem. : journal. - 1993. - Vol. 36 , no. 15 . - P. 2066-2074 . - DOI : 10.1021 / jm00067a003 . - PMID 8101876 .
↑ McCall RB, Romero AG, Bienkowski MJ, Harris DW, McGuire JC, Piercey MF, Shuck ME, Smith MW, Svensson KA, Schreur PJ, et al. Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. (English) // J Pharmacol Exp Ther. : journal. - 1994. - Vol. 271 , no. 2 . - P. 875-883 . - PMID 7965808 .
↑ Winter JC, Timineri D. The discriminative stimulus properties of EGb 761, an extract of Ginkgo biloba (Eng.) // Pharmacol. Biochem. Behav. : journal. - 1999 .-- March ( vol. 62 , no. 3 ). - P. 543-547 . - DOI : 10.1016 / S0091-3057 (98) 00190-7 . - PMID 10080249 .

[1] Winsauer PJ, Rodriguez FH, Cha AE, Moerschbaecher JM Full and partial 5-HT1A receptor agonists disrupt learning and performance in rats // J. Pharmacol. Exp. Ther. : journal. - 1999 .-- January ( vol. 288 , no. 1 ). - P. 335—347 . - PMID 9862788 .

[pmid1351756-2] Griebel G., Misslin R., Pawlowski M., Guardiola Lemaître B., Guillaumet G., Bizot-Espiard J. Anxiolytic-like effects of a selective 5-HT1A agonist, S20244, and its enantiomers in mice. (English) // Neuroreport. : journal. - 1992. - Vol. 3 , no. 1 . - P. 84-86 . - DOI : 10.1097 / 00001756-199201000-00022 . - PMID 1351756 .

[pmid1357709-3] Simon P., Guardiola B., Bizot-Espiard J., Schiavi P., Costentin J. 5-HT1A receptor agonists prevent in rats the yawning and penile erections induced by direct dopamine agonists. (Eng.) // Psychopharmacology : journal. - Springer , 1992. - Vol. 108 , no. 1-2 . - P. 47-50 . - DOI : 10.1007 / BF02245284 . - PMID 1357709 .

[pmid12505530-4] Astier B., Lambás Señas L., Soulière F., Schmitt P., Urbain N., Rentero N., Bert L., Denoroy L., Renaud B., Lesourd M., Muñoz C., Chouvet G. In vivo comparison of two 5-HT1A receptors agonists alnespirone (S-20499) and buspirone on locus coeruleus neuronal activity. (English) // Eur J Pharmacol. : journal. - 2003. - Vol. 459 , no. 1 . - P. 17-26 . - DOI : 10.1016 / S0014-2999 (02) 02814-5 . - PMID 12505530 .

[pmid12595749-5] Bardin L., Tarayre JP, Malfetes N., Koek W., Colpaert FC Profound, non-opioid analgesia produced by the high-efficacy 5-HT (1A) agonist F 13640 in the formalin model of tonic nociceptive pain ) // Pharmacology: journal. - 2003 .-- April ( vol. 67 , no. 4 ). - P. 182-194 . - DOI : 10.1159 / 000068404 . - PMID 12595749 .

[pmid12694810-6] Bruins Slot LA, Koek W., Tarayre JP, Colpaert FC Tolerance and inverse tolerance to the hyperalgesic and analgesic actions, respectively, of the novel analgesic, F 13640 (English) // European Journal of Pharmacology : journal. - 2003 .-- April ( vol. 466 , no. 3 ). - P. 271—279 . - DOI : 10.1016 / S0014-2999 (03) 01566-8 . - PMID 12694810 .

[pmid15528450-7] Bardin L., Assié MB, Pélissou M., Royer-Urios I., Newman-Tancredi A., Ribet JP, Sautel F., Koek W., Colpaert FC Dual, hyperalgesic, and analgesic effects of the high-efficacy 5 -hydroxytryptamine 1A (5-HT1A) agonist F 13640 [(3-chloro-4-fluoro-phenyl) - [4-fluoro-4 - {[(5-methyl-pyridin-2-ylmethyl) -amino] -methyl} piperidin-1-yl] methanone, fumaric acid salt]: relationship with 5-HT1A receptor occupancy and kinetic parameters (Eng.) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 2005 .-- March ( vol. 312 , no. 3 ). - P. 1034-1042 . - DOI : 10.1124 / jpet.104.077669 . - PMID 15528450 .

[pmid16254131-8] Colpaert FC, Deseure K., Stinus L., Adriaensen H. High-efficacy 5-hydroxytryptamine 1A receptor activation counteracts opioid hyperallodynia and affective conditioning (Eng.) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 2006 .-- February ( vol. 316 , no. 2 ). - P. 892-899 . - DOI : 10.1124 / jpet.105.095109 . - PMID 16254131 .

[pmid17512927-9] Deseure K., Bréand S., Colpaert FC Curative-like analgesia in a neuropathic pain model: parametric analysis of the dose and the duration of treatment with a high-efficacy 5-HT (1A) receptor agonist (eng.) // European Journal of Pharmacology : journal. - 2007 .-- July ( vol. 568 , no. 1-3 ). - P. 134-141 . - DOI : 10.1016 / j.ejphar.2007.04.0.022 . - PMID 17512927 .

[10] Bernard Vacher, Bernard Bonnaud, Wouter Koek. Pyridin-2-yl-methylamine derivatives, method of preparing and application as medicine. US Patent 6020345, May 21, 1999.

[pmid9765347-11] Koek W., Patoiseau JF, Assié MB, et al. F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential (English) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 1998 .-- October ( vol. 287 , no. 1 ). - P. 266-283 . - PMID 9765347 .

[pmid12398907-12] Prinssen EP, Colpaert FC, Koek W. 5-HT1A receptor activation and anti-cataleptic effects: high-efficacy agonists maximally inhibit haloperidol-induced catalepsy (English) // European Journal of Pharmacology : journal. - 2002. - October ( vol. 453 , no. 2-3 ). - P. 217-221 . - DOI : 10.1016 / S0014-2999 (02) 02430-5 . - PMID 12398907 .

[pmid17803293-13] Maurel JL, Autin JM, Funes P., Newman-Tancredi A., Colpaert F., Vacher B. High-efficacy 5-HT1A agonists for antidepressant treatment: a renewed opportunity ( Journal ) // Journal of Medicinal Chemistry : journal. - 2007 .-- October ( vol. 50 , no. 20 ). - P. 5024-5033 . - DOI : 10.1021 / jm070714l . - PMID 17803293 .

[pmid19154445-14] Newman-Tancredi A., Martel JC, Assié MB, et al. Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist (Eng.) // British Journal of Pharmacology : journal. - 2009 .-- January ( vol. 156 , no. 2 ). - P. 338-353 . - DOI : 10.1111 / j.1476-5381.2008.00001.x . - PMID 19154445 .

[pmid8026543-15] Haj-Dahmane S., Jolas T., Laporte AM, et al. Interactions of lesopitron (E-4424) with central 5-HT1A receptors: in vitro and in vivo studies in the rat // English Journal of Pharmacology : journal. - 1994 .-- April ( vol. 255 , no. 1-3 ). - P. 185-196 . - DOI : 10.1016 / 0014-2999 (94) 90097-3 . - PMID 8026543 .

[pmid9622555-16] Monte AP, Marona-Lewicka D., Lewis MM, Mailman RB, Wainscott DB, Nelson DL, Nichols DE Substituted naphthofurans as hallucinogenic phenethylamine-ergoline hybrid molecules with unexpected muscarinic antagonist activity (Eng.) // Journal of Medicinal Chemistry : journal. - 1998 .-- June ( vol. 41 , no. 12 ). - P. 2134-2145 . - DOI : 10.1021 / jm980076u . - PMID 9622555 .

[pmid7523657-17] Foreman MM, Fuller RW, Rasmussen K., Nelson DL, Calligaro DO, Zhang L., Barrett JE, Booher RN, Paget CJ, Flaugh ME Pharmacological characterization of LY293284: A 5-HT1A receptor agonist with high potency and selectivity .) // The Journal of Pharmacology and Experimental Therapeutics : journal. - 1994 .-- September ( vol. 270 , no. 3 ). - P. 1270-1281 . - PMID 7523657 .

[18] Matsuda T. , Yoshikawa T. , Suzuki M. , Asano S. , Somboonthum P. , Takuma K. , Nakano Y. , Morita T. , Nakasu Y. , Kim HS Novel benzodioxan derivative, 5- (3 - [( (2S) -1,4-benzodioxan-2-ylmethyl) amino propoxy) -1,3-benzodioxole HCl (MKC-242), with a highly potent and selective agonist activity at rat central serotonin1A receptors.] / / Japanese journal of pharmacology. - 1995. - Vol. 69, no. 4 . - P. 357-366. - PMID 8786639 .

[19] De Vry J. , Schohe-Loop R. , Heine HG , Greuel JM , Mauler F. , Schmidt B. , Sommermeyer H. , Glaser T. Characterization of the aminomethylchroman derivative BAY x 3702 as a highly potent 5-hydroxytryptamine1A receptor agonist . (Eng.) // The Journal of pharmacology and experimental therapeutics. - 1998. - Vol. 284, no. 3 . - P. 1082-1094. - PMID 9495870 .

[20] Dong J. , de Montigny C. , Blier P. Full agonistic properties of BAY x 3702 on presynaptic and postsynaptic 5-HT1A receptors electrophysiological studies in the rat hippocampus and dorsal raphe. (Eng.) // The Journal of pharmacology and experimental therapeutics. - 1998. - Vol. 286, no. 3 . - P. 1239-1247. - PMID 9732384 .

[pmid8101876-21] Romero AG, Leiby JA, McCall RB, Piercey MF, Smith MW, Han F. Novel 2-substituted tetrahydro-3H-benz [e] indolamines: highly potent and selective agonists acting at the 5-HT1A receptor as possible anxiolytics and antidepressants . (Eng.) // J Med Chem. : journal. - 1993. - Vol. 36 , no. 15 . - P. 2066-2074 . - DOI : 10.1021 / jm00067a003 . - PMID 8101876 .

[pmid7965808-22] McCall RB, Romero AG, Bienkowski MJ, Harris DW, McGuire JC, Piercey MF, Shuck ME, Smith MW, Svensson KA, Schreur PJ, et al. Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. (English) // J Pharmacol Exp Ther. : journal. - 1994. - Vol. 271 , no. 2 . - P. 875-883 . - PMID 7965808 .

[23] Winter JC, Timineri D. The discriminative stimulus properties of EGb 761, an extract of Ginkgo biloba (Eng.) // Pharmacol. Biochem. Behav. : journal. - 1999 .-- March ( vol. 62 , no. 3 ). - P. 543-547 . - DOI : 10.1016 / S0091-3057 (98) 00190-7 . - PMID 10080249 .