Talsaklidin

Talsaklidin
(IUPAC) ime
	(3R)-3-(prop-2-in-1-iloksi)-1-azabiciklo[2.2.2]oktan
Klinički podaci
Identifikatori
CAS broj	147025-53-4
ATC kod	nije dodeljen
PubChem	71792
ChemSpider	64819
UNII	1O8VSL798T
Hemijski podaci
Formula	C10H15NO
Mol. masa	165,23 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C10H15NO/c1-2-7-12-10-8-11-5-3-9(10)4-6-11/h1,9-10H,3-8H2/t10-/m0/s1 ; Key: XVFJONKUSLSKSW-JTQLQIEISA-N
Farmakokinetički podaci
Bioraspoloživost	70%
Vezivanje za proteine plazme	7%
Izlučivanje	Renal (86%)
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Talsaklidin (WAL-2014) je neselektivni agonist muskarinskog acetilholinskog receptora koji deluje kao pun agonist na M₁ podtipu, i kao parcijalni agonist na M₂ i M₃ podtipovima.^[4]^[5]^[6] On je bio u razvoju za lečenje Alchajmerove bolesti ali je pokazao samo umerenu do slabe efikastnosti na rezus majmunima i ljudima, respektivno.^[6]^[7] Moguće je da je to posledica niza od doze zavisnih nuspojava među kojima je povećana brzina srca i krvni pritisak, povišena salivacija, urinarna frekvencija i gorući osećaj nakon urinacije, povećana lakrimacija i nazalna sekrecija, abnormalna akomodacija, gorušica, uznemiren stomak kao i grčevi, mučnina, povraćanje, i dijareja, eksesivno znojenje, i palpitacija.^[8]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Ensinger HA, Doods HN, Immel-Sehr AR, et al. (1993). „WAL 2014--a muscarinic agonist with preferential neuron-stimulating properties”. Life Sciences 52 (5-6): 473–80. DOI:10.1016/0024-3205(93)90304-L. PMID 8441328.
↑ Walland A, Burkard S, Hammer R, Tröger W (1997). „In vivo consequences of M1-receptor activation by talsaclidine”. Life Sciences 60 (13-14): 977–84. DOI:10.1016/S0024-3205(97)00037-4. PMID 9121364.
↑ ^6,0 ^6,1 Wienrich M, Meier D, Ensinger HA, et al. (April 2001). „Pharmacodynamic profile of the M1 agonist talsaclidine in animals and man”. Life Sciences 68 (22-23): 2593–600. DOI:10.1016/S0024-3205(01)01057-8. PMID 11392631.
↑ Terry AV, Buccafusco JJ, Borsini F, Leusch A (July 2002). „Memory-related task performance by aged rhesus monkeys administered the muscarinic M(1)-preferring agonist, talsaclidine”. Psychopharmacology 162 (3): 292–300. DOI:10.1007/s00213-002-1105-3. PMID 12122487.
↑ Adamus WS, Leonard JP, Tröger W (1995). „Phase I clinical trials with WAL 2014, a new muscarinic agonist for the treatment of Alzheimer's disease”. Life Sciences 56 (11-12): 883–90. DOI:10.1016/0024-3205(95)00024-Z. PMID 10188789.

Povezano

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[pmid8441328-4] Ensinger HA, Doods HN, Immel-Sehr AR, et al. (1993). „WAL 2014--a muscarinic agonist with preferential neuron-stimulating properties”. Life Sciences 52 (5-6): 473–80. DOI:10.1016/0024-3205(93)90304-L. PMID 8441328.

[pmid9121364-5] Walland A, Burkard S, Hammer R, Tröger W (1997). „In vivo consequences of M1-receptor activation by talsaclidine”. Life Sciences 60 (13-14): 977–84. DOI:10.1016/S0024-3205(97)00037-4. PMID 9121364.

[pmid11392631-6] 6,0 ^6,1 Wienrich M, Meier D, Ensinger HA, et al. (April 2001). „Pharmacodynamic profile of the M1 agonist talsaclidine in animals and man”. Life Sciences 68 (22-23): 2593–600. DOI:10.1016/S0024-3205(01)01057-8. PMID 11392631.

[pmid12122487-7] Terry AV, Buccafusco JJ, Borsini F, Leusch A (July 2002). „Memory-related task performance by aged rhesus monkeys administered the muscarinic M(1)-preferring agonist, talsaclidine”. Psychopharmacology 162 (3): 292–300. DOI:10.1007/s00213-002-1105-3. PMID 12122487.

[pmid10188789-8] Adamus WS, Leonard JP, Tröger W (1995). „Phase I clinical trials with WAL 2014, a new muscarinic agonist for the treatment of Alzheimer's disease”. Life Sciences 56 (11-12): 883–90. DOI:10.1016/0024-3205(95)00024-Z. PMID 10188789.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]